620 articles for thisTarget
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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
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s
University of Catania
Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge.
Universit£
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds.
Mossakowski Medical Research Centre Polish Academy of Sciences
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.
Clinical Research Institute of Montreal
[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
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
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.
Vrije Universiteit Brussel
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
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
Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands.
University of Arizona
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
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.
University of Arizona
Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.
University of Arizona
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.
University of Arizona
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
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
'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode.
Clinical Research Institute of Montreal
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
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
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.
Vrije Universiteit Brussel
Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6a-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
Virginia Commonwealth University
Methoxyflavones from Stachys glutinosa with binding affinity to opioid receptors: in silico, in vitro, and in vivo studies.
National Research Council
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
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
Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine.
TBA
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.
Kitasato University
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University of Bath
Novel delta opioid receptor agonists with oxazatricyclodecane structure.
Kitasato University
In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt
Vrije Universiteit Brussel
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
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)
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.
Lanzhou University
Biological active analogues of the opioid peptide biphalin: mixeda/ß(3)-peptides.
Universit£
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
Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.
University of Naples
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
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: part 3, novel propellane derivatives with pentacyclic skeletons.
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
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
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
The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2.
Biological Research Center of The Hungarian Academy of Sciences
cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.
Universit£
Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associatedµ opioid receptor (MOR-1) splice variants.
Memorial Sloan-Kettering Cancer Center
A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).
Lanzhou University
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
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties.
Vrije Universiteit Brussel
Tuned-Affinity Bivalent Ligands for the Characterization of Opioid Receptor Heteromers.
TBA
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
The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues.
Universit£
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
Development of potent µ and d opioid agonists with high lipophilicity.
University of Arizona
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
University of Innsbruck and Center For Molecular Biosciences Innsbruck-Cmbi
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
University of Arizona
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute of Montreal
Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Kitasato University
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
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
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
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
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.
Toray Industries
Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
Vrije Universiteit Brussel
Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.
Stanford University School of Medicine
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
University of Ferrara
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
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
University of Maryland
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
University of Minnesota
Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
Biological Research Center of The Hungarian Academy of Sciences
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.
University of Maryland
Synthesis of bridged piperazines with sigma receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
Kyushu University
Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity.
Taisho Pharmaceutical
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.
University of Missouri-Columbia
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
Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide.
Tohoku Pharmaceutical University
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
University of Cagliari
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
New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Vrije Universiteit Brussels
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
University of Arizona
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Universit£
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
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
Universit£
18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
Technische Universit£T M£Nchen
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.
University of Arizona
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
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
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
Glaxosmithkline
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
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£
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
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
University of Cagliary
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
University of Cagliari
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
University of Innsbruck
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.
Research Triangle Institute
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance.
Universit£
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
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
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.
University of Lausanne
[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
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.
Clinical Research Institute of Montr£Al
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.
Rensselaer Polytechnic Institute
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.
University of Catania
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
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.
Uppsala University
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
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
University of Washington
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid r
National Institute of Diabetes and Digestive and Kidney Diseases
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.
University of Arizona
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
Smithkline Beecham
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.
University of Ferrara
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
University of Ferrara
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
Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity.
University of Minnesota
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
The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto
University of Arizona
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
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
Clinical Research Institute of Montreal
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
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library.
Chiron
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.
University of Minnesota
Newly discovered stereochemical requirements in the side-chain conformation of delta opioid agonists for recognizing opioid delta receptors.
University of Arizona
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
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.
University of Arizona
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
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
University of Arizona
Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine.
University of Minnesota
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
Clinical Research Institute of Montreal
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
Systemic analgesic activity and delta-opioid selectivity in [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin.
Searle Research and Development
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
Analogs of the delta opioid receptor selective cyclic peptide [2-D-penicillamine,5-D-penicillamine]-enkephalin: 2',6'-dimethyltyrosine and Gly3-Phe4 amide bond isostere substitutions.
G.D. Searle And
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
Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at sigma, PCP, and mu opioid receptors.
Research Triangle Institute
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
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
Synthesis and structure-activity relationships of deltorphin analogues.
University of Ferrara
Function of negative charge in the"address domain" of deltorphins.
National Institute of Environmental Health Sciences
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
University of Minnesota
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£
Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine.
University of Washington
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
University of Minnesota
Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.
University of Washington
[D-Pen2,D-Pen5]enkephalin analogues with increased affinity and selectivity for delta opioid receptors.
University of Arizona
Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity.
Ciba-Geigy
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.
Ciba-Geigy
Synthesis of highly mu and delta opioid receptor selective peptides containing a photoaffinity group.
University of Arizona
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
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
University of Paris
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.
Sri International
Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
TBA
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
University of Minnesota
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
TBA
Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
TBA
Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for mu or delta opiate receptors.
TBA
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.
TBA
Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides.
TBA
Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
TBA
Oral bioavailability of a new class of micro-opioid receptor agonists containing 3,6-bis[Dmt-NH(CH(2))(n)]-2(1H)-pyrazinone with central-mediated analgesia.
National Institutes of Environmental Health Sciences
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.
Southern Research Institute
Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.
University of Louisville
Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.
University of Bristol
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
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.
R. W. Johnson Pharmaceutical Research Institute
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
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.
Universit£
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
Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity.
Universit£
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
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.
University of Michigan
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Merck
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
Pyrrolooctahydroisoquinolines as potent and selective opioid receptor ligands: SAR analysis and docking studies
TBA
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
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.
Harvard Medical School
Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists.
Kitasato University
Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs.
Medical University of Lodz
Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.
University of Pavia
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.
University of Arizona
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
Synthesis, biological evaluation, and automated docking of constrained analogues of the opioid peptide H-Dmt-D-Ala-Phe-Gly-NH2 using the 4- or 5-methyl substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one scaffold.
Vrije Universiteit Brussel
Derivatives of pyrrolo[3,4-d]pyridazinone, a new class of analgesic agents.
Wroclaw Medical University
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
Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
University of Arizona
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
Hungarian Academy of Sciences
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
Kitasato University
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
Design and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration.
Kitasato University
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.
Sapienza University of Rome
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
University of Cagliari
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
University of Arizona
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
Kitasato University
Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues.
Universit£
Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans.
University of Debrecen
Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.
Vrije Universiteit Brussel
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
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.
Fudan University
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
University of Arizona
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 investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.
University of Arizona
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
The University of Kansas
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
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 pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
The University of Kansas
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
University of Cagliari
Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.
Kitasato University
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
Universit£
Akuammine and Dihydroakuammine, Two Indolomonoterpene Alkaloids Displaying Affinity for Opioid Receptors
TBA
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by alpha-aminoxy acids.
TBA
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
Specific affinity labeling of μ opioid receptors in rat brain by S-activated sulfhydryldihydromorphine analogs
TBA
Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs
TBA
Synthesis and biological properties of quaternized N-methylation analogs of D-Arg-2-dermorphin tetrapeptide
TBA
A new approach to enhance bioavailability of biologically active peptides: conjugation of a δ opioid agonist to β-cyclodextrin
TBA
The use of synthetic peptide combinatorial libraries for the determination of peptide ligands in radio-receptor assays: Opioid peptides
TBA
Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin I
TBA
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.
Medical University of Lodz
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.
Mclean Hospital
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.
Vrije Universiteit Brussel
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
National University of Singapore
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
University of Cagliari
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
Hungarian Academy of Sciences
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Lanzhou University
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
University of Queensland
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.
Medical University of Lodz
A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
University of Ferrara
Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.
Kobe Gakuin University
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
Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore.
University of Cagliari
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.
University of Arizona
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
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Medical University
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.
Taisho Pharmaceutical
Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Hungarian Academy of Sciences
Benzomorphan skeleton, a versatile scaffold for different targets: A comprehensive review.
University of Catania
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
University of Arizona
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Lanzhou University
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Kobe Gakuin University
Modified Akuamma Alkaloids with Increased Potency at the Mu-opioid Receptor.
University of Illinois Chicago
Oxidative Metabolism as a Modulator of Kratom's Biological Actions.
University of Health Sciences & Pharmacy and Washington University School of Medicine
Synthesis of 3,6-bis[H-Tyr/H-Dmt-NH(CH2)m,n]-2(1H)pyrazinone derivatives: function of alkyl chain length on opioid activity.
Kobe Gakuin University
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 evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
University of Arizona
6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
Universidad De Santiago De Compostela
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
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4.
Lanzhou University
Synthesis of 8-aminomorphans with high KOR affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Identification of potent phenyl imidazoles as opioid receptor agonists.
Johnson & Johnson Pharmaceutical Research & Development
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
University of Cagliari
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Kobe Gakuin University
Synthesis and biological activity of the first cyclic biphalin analogues.
University of Arizona
Is a Highly Selective and Potent ? Opioid Receptor (KOR) Agonist with an Unexpected Nonreduction in Locomotor Activity.
Fudan University
New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Kobe Gakuin University
From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.
University of Cagliari
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
Universit£
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
TBA
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
University of Catania
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.
University of Szeged
Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor.
Università
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
Lanzhou University
Modulating ?-arrestin 2 recruitment at the ?- and ?-opioid receptors using peptidomimetic ligands.
The Ohio State University
Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).
Kobe Gakuin University
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.
Kobe Gakuin University
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
University of Cagliary
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
University of The Punjab
Design, Synthesis, and Biological Evaluation of NAP Isosteres: A Switch from Peripheral to Central Nervous System Acting Mu-Opioid Receptor Antagonists.
Virginia Commonwealth University
Rational Design, Chemical Syntheses, and Biological Evaluations of Peripherally Selective Mu Opioid Receptor Ligands as Potential Opioid Induced Constipation Treatment.
Virginia Commonwealth University
Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists.
Johnson and Johnson Pharmaceutical Research and Development
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Johnson & Johnson Pharmaceutical Research & Development
Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
Virginia Commonwealth University
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Clinical Research Institute of Montreal
Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.
University of Cagliary
Optimization of bifunctional piperidinamide derivatives as ?
Huazhong University of Science and Technology
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
Kobe Gakuin University
Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the ?-Opioid Receptor for the Treatment of Chronic Abdominal Pain.
Medical University of Vienna
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
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
Harbin Institute of Technology
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
Exploring naltrexamine derivatives featuring azaindole moiety via nitrogen-walk approach to investigate their in vitro pharmacological profiles at the mu opioid receptor.
Virginia Commonwealth University
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
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.
Kobe Gakuin University
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
Rensselaer Polytechnic Institute
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.
Huazhong University of Science and Technology
Mechanism of action of the diazabicyclononanone-type kappa-agonists.
UniversitäT WüRzburg
Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.
Tohoku Pharmaceutical University
Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
Virginia Commonwealth University
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Crystal structures of dipeptides containing the Dmt-Tic pharmacophore.
National Institute of Environmental Health Sciences
Synthesis and structure-activity relationships of an orally available and long-acting analgesic peptide, N(alpha)-amidino-Tyr-D-Arg-Phe-MebetaAla-OH (ADAMB).
Daiichi Fine Chemical
Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.
Virginia Commonwealth University
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.
Institute For Molecular Studies
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
Design and synthesis of a bivalent probe targeting the putative mu opioid receptor and chemokine receptor CXCR4 heterodimer.
Virginia Commonwealth University
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Tohoku Pharmaceutical University
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
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
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
Lanzhou University
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
Tohoku Pharmaceutical University
Synthesis and evaluation of isothiocyanate-containing derivatives of the delta-opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP) as potential affinity labels for delta-opioid receptors.
University of Maryland
Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues.
Virginia Commonwealth University
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
Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit ?-Arrestin-2.
Memorial Sloan Kettering Cancer Center
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 and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.
R. W. Johnson Pharmaceutical Research 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
Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.
Hungarian Academy of Sciences
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.
Pfizer
Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.
University of Arizona
Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.
The University of Arizona
Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.
University of Louisville
Progress in the development of more effective and safer analgesics for pain management.
University of Catania
Further studies on the Dmt-Tic pharmacophore: hydrophobic substituents at the C-terminus endow delta antagonists to manifest mu agonism or mu antagonism.
University of Ferrara
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Synaptic Pharmaceutical
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
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
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
Sapienza University of Rome
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
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
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.
University of Arizona
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.
The University of Arizona
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
Research Triangle Institute
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
Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as ?/? Opioid Receptor Dual Selective Ligands.
Virginia Commonwealth University
7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.
University of Minnesota
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as antagonists of the NMDA receptor-channel complex.
Boehringer Ingelheim Pharmaceuticals
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Oregon State University
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.
National Institute of Environmental Health Sciences
Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators.
Virginia Commonwealth University
Discovery of a Highly Selective and Potent ? Opioid Receptor Agonist from
Fudan University
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
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
Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.
University of Arizona
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
Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides.
University of Ferrara
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
Discovery of Novel Multifunctional Ligands with ?/? Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.
University of Arizona
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
University of Arizona
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
Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site.
National Institute of Diabetes and Digestive and Kidney Diseases
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
University of Arizona
Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors.
University of Ferrara
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
Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration.
Medical University of Lodz
N-Alkyl dien- and trienamides from the roots of Otanthus maritimus with binding affinity for opioid and cannabinoid receptors.
Uos of Cagliari
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
Synthesis and biological evaluation of novel delta (?) opioid receptor ligands with diazatricyclodecane skeletons.
C.N.R. Istituto Di Farmacologia Traslazionale
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
Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation.
Universit£
Structure activity relationship studies of 17-cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affinity and function.
Virginia Commonwealth University
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
Development of a model for the delta opioid receptor pharmacophore. 2. Conformationally restricted Phe3 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
University of Michigan
Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).
University of Michigan
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
University of Arizona
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
Universit£
Synthesis and changes in affinity for NOP and opioid receptors of novel hexapeptides containing ?(2)-tryptophan analogues.
Bulgarian Academy of Sciences
Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.
Smithkline Beecham Farmaceutici
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
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 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
Stereoisomers of N-[1-hydroxy-(2-phenylethyl)-3-methyl-4-piperidyl]- N-phenylpropanamide: synthesis, stereochemistry, analgesic activity, and opioid receptor binding characteristics.
Institute of Materia Medica
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
Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties.
Tohoku College of Pharmacy
(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
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
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
Design and synthesis of naltrexone-derived affinity labels with nonequilibrium opioid agonist and antagonist activities. Evidence for the existence of different mu receptor subtypes in different tissues.
TBA
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
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
Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile.
Universit£
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl).
University of Kansas
Original endomorphin-1 analogues exhibit good analgesic effects.
The First Hospital of Lanzhou University
Design and synthesis of somatostatin analogues with topographical properties that lead to highly potent and specific mu opioid receptor antagonists with greatly reduced binding at somatostatin receptors.
University of Arizona
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
TBA
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
Ua 498 Cnrs
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic ? Receptor Ligands with Exocyclic Amino Moiety.
Universit£T M£Nster
Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position.
Clinical Research Institute of Montreal
New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties.
Boc Technical Center
Dermorphin analogues carrying an increased positive net charge in their"message" domain display extremely high mu opioid receptor selectivity.
Clinical Research Institute of Montreal
?-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.
Vrije Universiteit Brussel
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.
Anaquest Pharmaceuticals
Development of novel LP1-based analogues with enhanced delta opioid receptor profile.
University of Catania
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
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
Original endomorphin-1 analogues exhibit good analgesic effects with minimal implications for human sperm motility.
The Reproductive Medicine Special Hospital of The First Hospital of Lanzhou University
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
Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity.
Hebrew University of Jerusalem
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds.
Istituto Superiore Di Sanità
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.
Clinical Research Institute of Montreal
(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
Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.
University of Notre Dame
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
Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites.
University of Ferrara
Conformationally restricted deltorphin analogues.
Clinical Research Institute of Montreal
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity.
University of Arizona
Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.
Harvard Medical School
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors.
National Institute of Environmental Health Sciences
Synthesis and evaluation of a ligand targeting the? and? opioid receptors for drug delivery to lung cancer.
Purdue University
Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.
University of Maryland
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
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.
Taisho Pharmaceutical
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
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
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.
Pudue Pharma Discovery Research
Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor.
Taisho Pharmaceutical
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
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
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
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
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.
Glaxo Group Research
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
RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist.
Syntex Discovery Research
Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception.
R. W. Johnson Pharmaceutical Research Institute
Opioid binding properties of brain and peripheral tissues: evidence for heterogeneity in opioid ligand binding sites.
Stanford University
Characterization of the binding of a morphine (mu) receptor-specific ligand: Tyr-Pro-NMePhe-D-Pro-NH2, [3H]-PL17.
Burroughs Wellcome
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.
Nida Addiction Research Center
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
SDZ 205-557, a selective, surmountable antagonist for 5-HT4 receptors in the isolated guinea pig ileum.
Sandoz Pharma
Discovery and structure-activity relationships of 4-aminoquinazoline derivatives, a novel class of opioid receptor like-1 (ORL1) antagonists.
Nippon Shinyaku
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
University of Arizona Tucson
Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.
Universita Degli Studi
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
University of Arizona Tucson
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
University of Arizona Tucson