845 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues.
Medical University of Lodz
Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective¿-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Dr. August Wolff Gmbh & Co. Kg Arzneimittel
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.
West Virginia University School of Pharmacy
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.
The University of Newcastle
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s
University of Catania
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
University of Tsukuba
Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists.
National Health Research Institutes
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.
Clinical Research Institute of Montreal
Structural determinants of diphenethylamines for interaction with the¿ opioid receptor: Synthesis, pharmacology and molecular modeling studies.
University of Innsbruck
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
St. John'S University
[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.
Nanjing Medical University
Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacyµ-Opioid Receptor (MOR)/d-Opioid Receptor (DOR) Ligands.
University of Michigan
Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans.
Ironwood Pharmaceuticals
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral¿-opioid receptor agonists.
China Pharmaceutical University
Discovery of Potent and Selective Agonists ofd Opioid Receptor by Revisiting the"Message-Address" Concept.
Fudan University
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
Vrije Universiteit Brussel
Evaluation of N-substituent structural variations in opioid receptor profile of LP1.
University of Catania
Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.
Kitasato University
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University of Minnesota
Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.
University of Michigan
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
Medical University of Lodz
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
Medical University of Lodz
Multitarget opioid ligands in pain relief: New players in an old game.
University of Catania
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Potentµ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
Torrey Pines Institute For Molecular Studies
Further Optimization and Evaluation of Bioavailable, Mixed-Efficacyµ-Opioid Receptor (MOR) Agonists/d-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.
University of Michigan
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.
The University of Kansas
Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Mercachem
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists.
Harvard Medical School
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
University of Tsukuba
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen asd opioid receptor inverse agonists.
Kitasato University
Design, synthesis, and structure-activity relationship of novel opioid¿ receptor selective agonists:a-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
Kitasato University
Synthesis and analgesic activity of alkylated, reduced and constrained oligoheterocyclic peptidomimetic analogs of Leu-enkephalin.
University of Monastir
Synthesis and Pharmacology of a Novel¿ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton.
Kitasato University
Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.
Pharmacokinetics
Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists.
Pharmacokinetics
'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode.
Clinical Research Institute of Montreal
Potency enhancement of the¿-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.
University of Kansas Specialized Chemistry Center
Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities atµ (MOR),d (DOR), and¿ (KOR) Opioid Receptors.
Torrey Pines Institute For Molecular Studies
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Medical University of Lodz
C7ß-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.
University of Bath
Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
National Institute On Drug Abuse
Synthesis and biological evaluations of novel endomorphin analogues containinga-hydroxy-ß-phenylalanine (AHPBA) displaying mixedµ/d opioid receptor agonist andd opioid receptor antagonist activities.
Zhejiang University
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
Universit£
Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists.
Dr. Reddy'S Laboratories
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.
West Chester University
Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profile.
Research Triangle Institute
Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.
National Health Research Institutes
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted¿-opioid receptor agonists.
Westf£Lische Wilhelms-Universit£T M£Nster
Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2.
Medical University of Lodz
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
University of Bath
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Studies toward the Development of Antiproliferative Neoclerodanes from Salvinorin A.
The University of Kansas
Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine.
TBA
Synthesis and¿-opioid receptor activity of furan-substituted salvinorin A analogues.
The University of Kansas
Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.
The University of Mississippi
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.
Kitasato University
Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.
University of Mississippi
Combination of cyclohexane and piperazine based¿-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and evaluation of three structurally related¹8F-labeled orvinols of different intrinsic activities: 6-O-[¹8F]fluoroethyl-diprenorphine ([¹8F]FDPN), 6-O-[¹8F]fluoroethyl-buprenorphine ([¹8F]FBPN), and 6-O-[¹8F]fluoroethyl-phenethyl-orvinol ([¹8F]FPEO).
University of Oslo
Design and synthesis of quinolinopropellane derivatives with selectived opioid receptor agonism.
University of Tsukuba
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University of Bath
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
Astraea Therapeutics
Novel delta opioid receptor agonists with oxazatricyclodecane structure.
Kitasato University
Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity.
Nanjing Medical University
[Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/¿ opioid activity profile.
Nanjing Medical University
Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.
Eli Lilly
Development of a bioavailableµ opioid receptor (MOPr) agonist,d opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.
University of Michigan
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.
University of Medicine & Dentistry of New Jersey-Robert Wood Johnson Medical School (Umdnj-Rwjms)
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors.
Rensselaer Polytechnic Institute
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.
Lanzhou University
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacyµ opioid receptor (MOR) agonist/d opioid receptor (DOR) antagonist ligands.
University of Michigan
The effect of 17-N substituents on the activity of the opioid¿ receptor in nalfurafine derivatives.
Kitasato University
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.
Pfizer
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.
Eli Lilly
Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide.
University of Ferrara
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
National Institute of Neuroscienc
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.
Rensselaer Polytechnic Institute
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 3: synthesis of novel triplet drugs with the bis(epoxymethano) or bis(dimethylepoxymethano) structure (double-capped triplet).
Kitasato University
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
Kitasato University
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
The University of Sydney
Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at thed opioid receptor. Discovery of two highly potent and selectived opioid agonists.
Clinical Research Institute of Montreal
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.
University of Innsbruck
Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives as peripheral selectiveµ opioid receptor Agents.
Virginia Commonwealth University
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Vrije Universiteit Brussel
Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversibleµ opioid receptor antagonist effects.
University of Bristol
14-Alkoxy- and 14-acyloxypyridomorphinans:µ agonist/d antagonist opioid analgesics with diminished tolerance and dependence side effects.
Southern Research Institute
Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.
University of Bologna
cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.
Universit£
Identification of a duald OR antagonist/µ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
Janssen Research and Development
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
The University of Queensland
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties.
Vrije Universiteit Brussel
Synthesis of quinolinomorphinan derivatives as highly selectived opioid receptor ligands.
Kitasato University
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
Kitasato University
Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.
University of Maryland
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
Harvard Medical School
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
Kitasato University
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Kitasato University
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
Kitasato University
Generation of novel radiolabeled opiates through site-selective iodination.
Memorial Sloan-Kettering Cancer Center
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.
National Institute of Mental Health
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic.
University of Cagliari
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
University of Sydney
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
University of Innsbruck and Center For Molecular Biosciences Innsbruck-Cmbi
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists.
Kitasato University
Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.
Research Triangle Institute
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Wilhelms-Universit£T M£Nster
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute of Montreal
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Kitasato University
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
Human Biomolecular Research Institute
Synthesis and opioid receptor activity of indolopropellanes.
Chinese Academy of Sciences
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Kitasato University
Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
Kitasato University
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Adolor
Syntheses of novel high affinity ligands for opioid receptors.
Rensselaer Polytechnic Institute
14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
Virginia Commonwealth University
Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.
Harvard Medical School
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
Universit£T Des Saarlandes
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
University of Bath
Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
Kitasato University
Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug.
Pfizer
Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
Virginia Commonwealth University
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Adolor
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Rensselaer Polytechnic Institute
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology.
Kitasato University
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
Toray Industries
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.
Toray Industries
Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis.
Torrey Pines Institute For Molecular Studies
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.
Purdue University
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Rensselaer Polytechnic Institute
Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
Development of potent and selective small-molecule human Urotensin-II antagonists.
Glaxosmithkline
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
Adolor
Herkinorin analogues with differential beta-arrestin-2 interactions.
The University of Iowa
Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.
Westf£Lische Wilhelms-Universit£T
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Harvard Medical School
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Mclean Hospital
Identification of novel benzimidazole series of potent and selective ORL1 antagonists.
Banyu Tsukuba Research Institute
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
University of Minnesota
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.
Institute
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.
University of Maryland
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Eli Lilly
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
University of Bath
Synthesis of bridged piperazines with sigma receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
The University of Iowa
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Schering-Plough Research Institute
High-affinity carbamate analogues of morphinan at opioid receptors.
Harvard Medical School
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
Harvard Medical School
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.
University of Missouri-Columbia
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.
University of Bath
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
Adolor
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
Adolor
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
University of Bristol
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.
Rensselaer Polytechnic Institute
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
University of Bristol
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.
University of Kentucky
Discovery of novel triazole-based opioid receptor antagonists.
University of Medicine and Dentistry of New Jersey and Umdnj Informatics Institute
A highly selective kappa-opioid receptor agonist with low addictive potential and dependence liability.
Kaist
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Harvard Medical School
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.
Sapienza University of Rome
Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.
University of Innsbruck
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
University of Bath
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
Rensselaer Polytechnic Institute
Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.
Harvard Medical School
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
Mclean Hospital
1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.
Purdue Pharma
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
Harvard Medical School
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Southern Research Institute
Importance of phenolic address groups in opioid kappa receptor selective antagonists.
Research Triangle Institute
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
Abbott Laboratories
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.
University of Innsbruck
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
University of Bath
2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists.
Harvard University
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
University of Bath
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Harvard Medical School
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.
University of Bath
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.
University of Innsbruck
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.
Universit£
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
University of Bath
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Research Triangle Institute
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.
University of Vermont
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
University of California
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
Research Triangle Institute
The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.
Universit£
Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.
TBA
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
University of Innsbruck
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
Universit£
4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.
University of Bristol
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.
Research Triangle Institute
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
National Institute of Diabetes and Digestive and Kidney Diseases
Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).
University of Minnesota
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
Research Triangle Institute
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the"address" recognition locus.
University of Minnesota
From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.
Universities of Lille
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
Clinical Research Institute of Montreal
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies.
Pharmazeutisches Institut Der Universit£T Freiburg
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Research Triangle Institute
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.
University of Minnesota
Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.
University of Bristol
Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.
University of Minnesota
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
F. Hoffmann-La Roche
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
University of Minnesota
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.
University of Minnesota
Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.
University of Bristol
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.
Rensselaer Polytechnic Institute
3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.
University of Bristol
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.
University of Catania
[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
University of California
Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.
University of Minnesota
Modeling of kappa-opioid receptor/agonists interactions using pharmacophore-based and docking simulations.
Universit£
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
Harvard Medical School
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.
National Institute of Diabetes
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Mixture-based synthetic combinatorial libraries.
Torrey Pines Institute For Molecular Studies
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Southern Research Institute
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Research Triangle Institute
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.
Vrije Universiteit Brussel
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.
University of Minnesota
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.
University of Minnesota
3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy.
University of Bristol
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.
Southern Research Institute
Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.
University of California San Diego
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
University of Washington
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.
University of Minnesota
Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide"address" recognition at kappa opioid receptors.
University of Minnesota
Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.
University of Minnesota
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
National Institute of Diabetes and Digestive and Kidney Diseases
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.
Research Triangle Institute
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
University of Washington
7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice.
University of Minnesota
Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime.
University of Innsbruck
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.
University of Minnesota
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
University of Washington
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.
Virginia Commonwealth University
Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.
University of Washington
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.
University of Minnesota
14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties.
Institute
Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor.
University of Minnesota
A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists.
University of Minnesota
Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity.
University of Minnesota
A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
Glaxo Group Research
A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists.
University of Minnesota
Substitution on the Phe3 aromatic ring in cyclic delta opioid receptor-selective dermorphin/deltorphin tetrapeptide analogues: electronic and lipophilic requirements for receptor affinity.
University of Michigan
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Oregon State University
O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
University of Washington
Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, delta opioid receptor selective tetrapeptide (JOM-13) enhances delta receptor binding affinity and selectivity.
University of Michigan
Opioid agonist and antagonist activities of morphindoles related to naltrindole.
University of Minnesota
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.
Zambeletti Research Laboratories
Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluation, and radiochemistry of [125I]-6 beta-iodo
National Institute of Diabetes and Digestive and Kidney Diseases
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
University of Washington
Selective reversible and irreversible ligands for the kappa opioid receptor.
National Taiwan University
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.
National Institute of Diabetes and Digestive and Kidney Diseases
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
University of Minnesota
Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
University of Minnesota
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
University of Minnesota
Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists.
Ici Pharmaceuticals Group
Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.
Parke-Davis Research Unit
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
Universit£
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
University of Minnesota
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.
National Institute of Diabetes and Digestive and Kidney Diseases
Highly selective kappa-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted-cyclohexyl]arylacetamide derivatives.
Parke-Davis Research Unit
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
National Institute of Digestive
Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.
Parke-Davis Research Unit
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.
Ciba-Geigy
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
Smith Kline and French Laboratories
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.
Parke-Davis Research Unit
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
Eli Lilly
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.
Sri International
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
TBA
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
Sri International
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.
Southern Research Institute
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.
Adolor
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
Schering-Plough Research Institute
Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.
University of Bristol
Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.
Niddk
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Harvard Medical School
3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.
Pharmacia
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.
F. Hoffmann-La Roche
Synthesis of enantiomerically pure (+)- and (-)-18-methoxycoronaridine hydrochloride and their preliminary assessment as anti-addictive agents.
Albany Molecular Research
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.
University of Maryland
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.
University of Bristol
Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.
Organon Laboratories
Delta opioid binding selectivity of 3-ether analogs of naltrindole.
National Institute of Diabetes
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
Research Triangle Institute
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
Research Triangle Institute
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.
National Institute of Diabetes
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.
University of Michigan
Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.
Institute For Bioorganic Research
Synthesis and biological evaluation of 14-alkoxymorphinans. 14.1 14-ethoxy-5-methyl substituted indolomorphinans with opioid receptor selectivity
TBA
Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the -selective opioid receptor antagonist cyprodime
TBA
EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists
TBA
Neurotensin receptor binding and antinociceptive activity for lipophilic N-amido neurotensin(913) analogs
TBA
Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selectiveµ-antagonist activity.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
¿-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.
Astrazeneca R&D Montreal
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.
Harvard Medical School
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.
Institute of Radiopharmacy
Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists.
Kitasato University
Discovery of aminobenzyloxyarylamides as¿ opioid receptor selective antagonists: application to preclinical development of a¿ opioid receptor antagonist receptor occupancy tracer.
Eli Lilly
Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.
University of Pavia
Discovery of isoxazole analogues of sazetidine-A as selectivea4ß2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.
University of Illinois At Chicago
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
Kitasato University
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
University of Bath
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.
The University of Sydney
Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.
Virginia Commonwealth University
Design and discovery of a selective small molecule¿ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).
Pfizer
Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens.
The University of Mississippi
Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
Kitasato University
Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.
Vrije Universiteit Brussel
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.
Harvard Medical School
Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.
University of Iowa
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.
Istituto Superiore Di Sanit£
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
Probes for narcotic receptor mediated phenomena. 41. Unusual inverseµ-agonists and potentµ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.
National Institute On Drug Abuse
Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.
University of Innsbruck
Synthesis, pharmacological activity and structure affinity relationships of spirocyclics(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.
University of Mississippi
Design and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration.
Kitasato University
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute of Mental Health
Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A.
Harvard Medical School
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.
Astrazeneca Pharmaceuticals
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.
Sapienza University of Rome
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.
Hokkaido University
SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
Astrazeneca Pharmaceuticals
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.
Purdue University
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
Kitasato University
Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Griffith University
Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Harvard Medical School
Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.
Kyorin Pharmaceutical
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Amgen
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.
Schering-Plough Research Institute
Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.
National Institute of Mental Health
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Pfizer
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
Kitasato University
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
University of Pavia
Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-ols.
Nida
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.
Pfizer
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.
Fudan University
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.
Institute of Chemical Biology
Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines.
National Taiwan University
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Harvard Medical School
N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: the development of diaryl amino piperidines as potent delta opioid receptor agonists with in vivo anti-nociceptive activity in rodent models.
Astrazeneca R & D Montr£Al
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO.
Biomedizinische Forschungsreagenzien
Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
Harvard Medical School
Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphans.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholi
14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.
University of Bristol
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
Clinical Research Institute of Montreal
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
University of Kansas
Delta agonist hydroxy bioisosteres: the discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stability.
Astrazeneca R & D Montr£Al
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.
University of Michigan
Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands.
Institute For Molecular Studies
Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
University of New England
Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
The University of Kansas
Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Adolor
Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.
Kitasato University
Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.
Tsukuba Research Institute
Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.
Tsukuba Research Institute
trans N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonists
TBA
6N-Cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions
TBA
Synthesis and opioid binding properties of 2-chloroacrylamido derivatives of 7,8-dihydromorphinans
TBA
Suppression of morphine and cocaine self-administration in rats by a mixed mu antagonist-kappa agonist (N-CBM-TAMO) and a long-acting selective D1 antagonist (AS-300)
TBA
Stereoselective synthesis and evaluation of all stereoisomers of Z4349, a novel and selective μ-opioid analgesic
TBA
Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists
TBA
N-Methyl and N-cyclopropylmethyl-14α,14′β-[dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis(7,8-dihydro-5β-methyl-morphinone) MET-TAMO and N-CPM-MET-TAMO: Synthesis and opioid binding properties
TBA
Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs
TBA
Preparation and evaluation of some hydrophilic phenylacetyl-piperazines as peripherally selective κ-opioid receptor agonists
TBA
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.
University of Toronto
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.
Mclean Hospital
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.
Rensselaer Polytechnic Institute
Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of the ortho- and para-d-isomers.
National Institute On Drug Abuse
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
National University of Singapore
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.
Harvard Medical School
A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.
Tsukuba Research Institute
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Glaxosmithkline
Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
Tsukuba Research Institute
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Institut FüR Pharmazeutische Und Medizinische Chemie
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Banyu Tsukuba Research Institute
Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.
University of Maryland
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: semisynthesis of salvinicins A and B and other chemical transformations of salvinorin A.
The University of Iowa
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.
National Institute of Mental Health
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position.
Holden Laboratories
Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Eli Lilly
Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
National Institute On Drug Abuse
Functionalization of the 6,14-bridge of the orvinols. Part 3: preparation and pharmacological evaluation of 18- and 19-hydroxyl substituted orvinols.
University of Maryland
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action.
Dipartimento Di Scienze Farmaceutiche
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective delta-opioid agonists with potential anxiolytic/antidepressant properties. Part 2.
Johnson & Johnson Pharmaceutical Research & Development
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Kobe Gakuin University
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.
Chinese Academy of Sciences
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Harvard Medical School
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Schering-Plough Research Institute
Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Clinical Research Institute of Montreal
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
University of Mississippi
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
Schering-Plough Research Institute
Benzomorphan skeleton, a versatile scaffold for different targets: A comprehensive review.
University of Catania
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.
Organon Laboratories
A review of salvinorin analogs and their kappa-opioid receptor activity.
The Scripps Research Institute
Conopeptide-Derived ?-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties.
Xenome
Modified Akuamma Alkaloids with Increased Potency at the Mu-opioid Receptor.
University of Illinois Chicago
Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.
National Institute of Diabetes & Digestive & Kidney Diseases
Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.
Harvard Medical School
New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
Harvard Medical School
Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
National University of Singapore
Discovery, Structure-Activity Relationship, and Mechanistic Studies of 1-((3
Fudan University
Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18).
Mclean Hospital
Identification of potent and highly selective chiral tri-amine and tetra-amine mu opioid receptors ligands: an example of lead optimization using mixture-based libraries.
Institute For Molecular Studies
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
Johnson & Johnson Pharmaceutical Research and Development
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring.
The University of Iowa
Synthesis of 8-aminomorphans with high KOR affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
Banyu Tsukuba Research Institute
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists.
Adolor
Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward ? and ? opioid receptors.
Kitasato University
Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor agonists.
Adolor
Is a Highly Selective and Potent ? Opioid Receptor (KOR) Agonist with an Unexpected Nonreduction in Locomotor Activity.
Fudan University
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.
Johnson and Johnson Pharmaceutical Research and Development
Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.
Adolor
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Johnson & Johnson Pharmaceutical Research and Development
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Columbia University College of Physicians and Surgeons
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
Universit£
Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
University of Tsukuba
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.
Harvard Medical School
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
The University of Iowa
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
TBA
Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.
Adolor
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
University of Trieste
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists.
Adolor
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.
The University of Melbourne
Conformational Constraint between Aromatic Residue Side Chains in the "Message" Sequence of the Peptide Arodyn Using Ring Closing Metathesis Results in a Potent and Selective Kappa Opioid Receptor Antagonist.
The University of Kansas
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
University of The Punjab
Rational Design, Chemical Syntheses, and Biological Evaluations of Peripherally Selective Mu Opioid Receptor Ligands as Potential Opioid Induced Constipation Treatment.
Virginia Commonwealth University
Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.
Adolor
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Emory University
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Johnson & Johnson Pharmaceutical Research & Development
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, biological, and structural explorations of a series of ?-opioid receptor (MOR) agonists with high G protein signaling bias.
Yantai University
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Clinical Research Institute of Montreal
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.
Lanzhou University
Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.
University of Innsbruck
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
Sri International
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
Harbin Institute of Technology
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from
Universidad Nacional Aut£Noma De M£Xico
Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2.
Vrije Universiteit Brussel
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Bristol Myers Squibb
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Biological Research Center of The Hungarian Academy of Sciences
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
University of Maryland
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
Harvard Medical School
Isolation and Pharmacological Characterization of Six Opioidergic
University of Illinois At Chicago
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.
University of Maryland
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.
Purdue Pharma
Neuropeptide FF and Its Receptors: Therapeutic Applications and Ligand Development.
Research Triangle Institute
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
Rensselaer Polytechnic Institute
New scaffolds in the development of mu opioid-receptor ligands.
Astrazeneca R&D Montreal
Mechanism of action of the diazabicyclononanone-type kappa-agonists.
UniversitäT WüRzburg
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.
University of Maryland
Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods.
Astrazeneca R&D
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist.
Shanghai Hengrui Pharmaceutical
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.
University of Maryland
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
Soochow University
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting ? Opioid Analgesic with Reduced Abuse Liability.
The University of Kansas
Structure-Based Optimization of Multifunctional Agonists for Opioid and Neuropeptide FF Receptors with Potent Nontolerance Forming Analgesic Activities.
Lanzhou University
Kappa-opioid receptor model in a phospholipid bilayer: molecular dynamics simulation.
University of Catania
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.
Institute For Molecular Studies
Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.
Shire Biochem
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.
University of Maryland
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.
University of California
3-Pyrroline containing arylacetamides: a novel series of remarkably selective kappa-agonists.
Chinese Academy of Sciences
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.
Lanzhou University
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
Vrije Universiteit Brussel
Synthesis, biochemical, pharmacological characterization and in silico profile modelling of highly potent opioid orvinol and thevinol derivatives.
University of Szeged
Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic.
Fudan University
3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.
Astrazeneca R&D MöLndal
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.
Niddk
Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent ?/? Opioid Agonists and Peripherally Selective Antinociceptives.
TBA
Synthesis and Structure-Activity Relationships of 5'-Aryl-14-alkoxypyridomorphinans: Identification of a ? Opioid Receptor Agonist/? Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects.
University of Alabama At Birmingham
Discovery of ? opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.
Kitasato University
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
Lanzhou University
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
Astrazeneca
Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
Astrazeneca R&D Montreal
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
Columbia University College of Physicians and Surgeons
Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective ? opioid receptor antagonists.
China Pharmaceutical University
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.
Universit£
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
Clinical Research Institute of Montreal
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
Central Pharmaceutical Research Institute
N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.
Astrazeneca R&D Montreal
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
Astrazeneca R&D Montreal
Synthesis and opioid receptor affinity of a series of 2, 4-diaryl-substituted 3,7-diazabicylononanones.
University of WüRzburg
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis:
Universit£
Dual Pharmacophores Explored via Structure-Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design.
TBA
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.
University of Minnesota
An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain.
University of Catania
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).
University of Bologna
4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.
Research Triangle Institute
Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.
Istituto Di Chimica Farmaceutica E Tossicologica
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).
The Scripps Research Institute
Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (?
Memorial Sloan Kettering Cancer Center
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.
Pfizer
Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.
Astrazeneca R&D MontréAl
Discovery of Axelopran (TD-1211): A Peripherally Restricted ?-Opioid Receptor Antagonist.
Theravance Biopharma Us
Progress in the development of more effective and safer analgesics for pain management.
University of Catania
Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.
University of Illinois At Chicago
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.
Universit£
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
Clinical Research Institute of Montreal
Endomorphin-2 analogs containing modified tyrosines: Biological and theoretical investigation of the influence on conformation and pharmacological profile.
Medical University of Lodz
Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and ?
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.
TBA
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina At Chapel Hill
Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.
Organon Laboratories
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.
Universit£T M£Nster
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic ?-Opioid Receptor (MOR) Agonist/?-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.
University of Michigan
Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy ?-Opioid Receptor (MOR)/?-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.
University of Michigan
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
University of Florida
Development of Novel Quinoxaline-Based ?-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
Universit£T M£Nster
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
Research Triangle Institute
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Bristol-Myers Squibb
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.
National Taiwan University
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors.
Biological Research Centre of The Hungarian Academy of Sciences
Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models.
Astraea Therapeutics
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
Research Triangle Institute
Investigation of Inactive-State ? Opioid Receptor Homodimerization via Single-Molecule Microscopy Using New Antagonistic Fluorescent Probes.
Julius Maximilian University of W£Rzburg
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Research Triangle Institute
(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.
University of Catania
Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.
Eisai
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Oregon State University
Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake.
Research Triangle Institute
Discovery of a Highly Selective and Potent ? Opioid Receptor Agonist from
Fudan University
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence.
Oregon State University
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
Hungarian Academy of Sciences
Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1(3-aminophenyl)-2-(1-pyrrolidi nyl) ethyl]acetamide: kappa opioid receptor agonists with limited access to the central nervous system.
University of Minnesota
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
University of Arizona
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
University of Arizona
Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids.
Institute
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Universitá
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Hoechst-Roussel Pharmaceuticals
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Synthesis of tripeptides containing D-Trp substituted at the indole ring, assessment of opioid receptor binding and in vivo central antinociception.
University of Bologna
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
Eli Lilly
Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
Eli Lilly
Potential Drug Abuse Therapeutics Derived from the Hallucinogenic Natural Product Salvinorin A.
University of Kansas
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Solvay Duphar
Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity ? opioid receptor (MOR) agonist/? opioid receptor (DOR) antagonist ligands.
University of Michigan
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice.
University of Minnesota
The most effective influence of 17-(3-ethoxypropyl) substituent on the binding affinity and the agonistic activity in KNT-127 derivatives, ? opioid receptor agonists.
Kitasato University
Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
Virginia Commonwealth University
Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.
Harvard Medical School
4?-Methyl-5-(3-hydroxyphenyl)morphan opioid agonist and partial agonist derived from a 4?-methyl-5-(3-hydroxyphenyl)morphan pure antagonist.
Research Triangle Institute
Structure-activity relationships and discovery of a G protein biased ? opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.
Trevena
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid.
Oregon State University
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
University of Arizona
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.
Eli Lilly
4-[(Alkylamino)methyl]furo[3,2-c]pyridines: a new series of selective kappa-receptor agonists.
Glaxo Group Research
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.
Clinical Research Institute of Montreal
Access to 7?-analogs of codeine with mixed ?/? agonist activity via 6,7-?-epoxide opening.
University of Texas At Austin
Probes for narcotic receptor mediated phenomena. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors.
University of Maryland
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
University of Arizona
Sandmeyer reaction repurposed for the site-selective, non-oxidizing radioiodination of fully-deprotected peptides: studies on the endogenous opioid peptide ?-neoendorphin.
Memorial Sloan-Kettering Cancer Center
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
Universit£
Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
Virginia Commonwealth University
A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.
National Taiwan University
Enkephalin analogs as systemically active antinociceptive agents: O- and N-alkylated derivatives of the dipeptide amide L-2,6-dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide.
Searle
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton having a 7-amide side chain and their pharmacologies.
Kitasato University
Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2.
University of Arizona
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.
University of Mississippi
kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists.
University of Minnesota
Electrophilic N-benzylnaltrindoles as delta opioid receptor-selective antagonists.
University of Minnesota
Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids.
Eastern Michigan University
14 beta-[(p-nitrocinnamoyl)amino]morphinones, 14 beta-[(p-nitrocinnamoyl)amino]-7,8-dihydromorphinones, and their codeinone analogues: synthesis and receptor activity.
Institute
Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.
University of Arizona
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 1. Conformational constraint in the"message" sequence.
Oregon State University
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
Design, Synthesis, and Preclinical Efficacy of Novel Nonretinoid Antagonists of Retinol-Binding Protein 4 in the Mouse Model of Hepatic Steatosis.
Albany College of Pharmacy and Health Sciences
Natural products as tools for neuroscience: discovery and development of novel agents to treat drug abuse.
University of Kansas
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties.
Organon Laboratories
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.
University of Minnesota
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
TBA
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.
University of Bath
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.
F. Hoffmann-La Roche
Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands.
Chiba University
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Texas Tech University Health Sciences Center
Selective kappa opioid antagonists for treatment of addiction, are we there yet?
University of Science and Technology
7?-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues.
Fudan University
O6C-20-nor-salvinorin A is a stable and potent KOR agonist.
The Scripps Research Institute
Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.
University of Catania
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.
TBA
Semisynthesis and Kappa-Opioid Receptor Activity of Derivatives of Columbin, a Furanolactone Diterpene.
Istanbul Technical University
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl).
University of Kansas
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
TBA
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic ? Receptor Ligands with Exocyclic Amino Moiety.
Universit£T M£Nster
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
Constraining Endomorphin-1 by ?,?-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel ?-Opioid Receptor Selective Partial Agonist.
University of Bologna
Synthesis and Evaluation of a Novel Bivalent Selective Antagonist for the Mu-Delta Opioid Receptor Heterodimer that Reduces Morphine Withdrawal in Mice.
TBA
Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets.
University of California San Francisco
Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.
University of Arizona
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
Development of novel LP1-based analogues with enhanced delta opioid receptor profile.
University of Catania
Discovery of highly selective?-opioid receptor agonists: 10?-Hydroxy TRK-820 derivatives.
Toray Industries
Addressing Structural Flexibility at the A-Ring on Salvinorin A: Discovery of a Potent Kappa-Opioid Agonist with Enhanced Metabolic Stability.
The University of Kansas
Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor.
University of Southern California
Design, synthesis and biological evaluation of aminobenzyloxyarylamide derivatives as selective? opioid receptor antagonists.
China Pharmaceutical University
Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
University of Arizona
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.
Eisai
Modification of the enkephalin"message" with an artificial polycationic C-terminus.
Case Western Reserve University
Antitrichomonal activity of? opioid receptor antagonists, 7-benzylidenenaltrexone derivatives.
University of Tsukuba
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.
Anaquest
(2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics.
Zambeletti Research Laboratories
2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists.
Ici Pharmaceuticals Group
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.
National Institute of Diabetes and Digestive and Kidney Diseases
Design and characterization of opioid ligands based on cycle-in-macrocycle scaffold.
Medical University of Lodz
Modulation of opioid receptor affinity and efficacy via N-substitution of 9?-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study.
National Institute On Drug Abuse and The National Institute On Alcohol Abuse
Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor.
The Scripps Research Institute
Design and synthesis of novel? opioid receptor agonists with an azatricyclodecane skeleton for improving blood-brain barrier penetration.
Nippon Chemiphar
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.
Zambeletti Research Laboratories
Novel delta opioid receptor agonists with oxazatricyclodecane structure showing potent agonistic activities.
Kitasato University
Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
University of Washington
Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent?-Opioid Receptor Agonists.
University of Innsbruck
Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of?-opioid receptor antagonists.
Theravance Biopharma Us
Effect of modification of the basic residues of dynorphin A-(1-13) amide on kappa opioid receptor selectivity and opioid activity.
Oregon State University
Preparation and opioid activity of analogues of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide.
G.D. Searle And
Highly Potent and Selective New Diphenethylamines Interacting with the?-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships.
University of Innsbruck
Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.
Harvard Medical School
New kappa-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus.
Glaxo Group Research
Chemotype-selective modes of action of ¿-opioid receptor agonists.
University of North Carolina
Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at kappa-opioid receptors in striatal neurons.
The Scripps Research Institute
Novel 2(3H)-benzothiazolones as highly potent and selective sigma-1 receptor ligands
Universite De Lille
Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.
Case Western Reserve University
Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.
Adolor
Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.
University of Maryland
Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
Human Biomolecular Research Institute
Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.
Columbia University
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.
Mcgill University
Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties.
University of Rochester
Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.
Case Western Reserve University
[(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.
Section of Pharmacology
Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.
Temple University
Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine.
Memorial Sloan-Kettering Cancer Center
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
Sanofi-Synthelabo Recherche
DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.
Purdue Pharma Discovery Research
FE200041 (D-Phe-D-Phe-D-Nle-D-Arg-NH2): A peripheral efficacious kappa opioid agonist with unprecedented selectivity.
University of Arizona
In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone.
University of Innsbruck
Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors.
Cornell University
Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist.
University of Innsbruck
Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.
University of Michigan
Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.
Case Western Reserve University
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.
Case Western Reserve University
Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.
Eli Lilly
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
Case Western Reserve University
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.
WestfÄLische Wilhelms-UniversitÄ
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
Novartis Pharma
Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.
Eli Lilly
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.
Case Western Reserve University
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Janssen Research Foundation
Dynorphin A analogs containing a conformationally constrained phenylalanine derivative in position 4: reversal of preferred stereochemistry for opioid receptor affinity and discrimination of kappa vs. delta receptors.
University of Maryland
Characterisation and comparison of novel ligands for the nociceptin/orphanin FQ receptor.
Leicester Royal Infirmary
Synthesis and in vitro opioid activity profiles of DALDA analogues.
Clinical Research Institute of Montreal
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Abbott Laboratories
Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.
Hungarian Academy of Sciences
Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group.
Loughborough University
Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.
Hungarian Academy of Sciences
Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity.
University of Rochester
Interaction of agonist peptide [3H]Tyr-D-Ala-Phe-Phe-NH2 with mu-opioid receptor in rat brain and CHO-mu/1 cell line.
Hungarian Academy of Sciences
Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain.
Memorial Sloan-Kettering Cancer Center
Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Sri International
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.
Roche Bioscience
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Janssen Research Foundation
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.
Abbott Laboratories
Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.
Vrije Universiteit
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
University of Pennsylvania
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.
Glaxo Group Research
Biochemical and pharmacological characterization of mu, delta and kappa 3 opioid receptors expressed in BE(2)-C neuroblastoma cells.
Memorial Sloan-Kettering Cancer Center
Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.
Yamanouchi Pharmaceutical
Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception.
R. W. Johnson Pharmaceutical Research Institute
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.
Nida Addiction Research Center
Characterization of kappa 1 and kappa 2 opioid binding sites in frog (Rana esculenta) brain membrane preparation.
Biological Research Center of Hungarian Academy of Sciences
Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.
Center For Bio-Pharmaceutical Sciences
Discovery and structure-activity relationships of 4-aminoquinazoline derivatives, a novel class of opioid receptor like-1 (ORL1) antagonists.
Nippon Shinyaku
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: part 2.
Schering-Plough Research Institute
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
Istituto Superiore Di Sanita