317 articles for thisTarget
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Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues.
Medical University Of Lodz
(+)-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£
Assessment of the in vivo and in vitro opioid activity of bridged hexahydroaporphine and isoquinoline molecules.
Creighton University
Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines.
Anaquest Pharmaceuticals
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
University Of Innsbruck
Probes for narcotic receptor mediated phenomena. 12. cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for delta opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity.
TBA
Probes for narcotic receptor mediated phenomena. 9. Synthesis of (+/-)-(3 alpha,6a alpha,11a beta)-1,3,4,5,6,11a-hexahydro-2-methyl-2H-3,6a- methanobenzofuro[2,3-c]azocin-10-ol, an oxide-bridged 5-(m-hydroxyphenyl)morphan.
TBA
Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydronororipavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistry, biochemistry, and pharmacology.
TBA
Irreversible blockage of opioid receptor types by ester homologues of beta-funaltrexamine.
TBA
Opioid agonists and antagonists. 6-Desoxy-6-substituted lactone, epoxide, and glycidate ester derivatives of naltrexone and oxymorphone.
TBA
Novel nonnarcotic analgesics with an improved therapeutic ratio. Structure-activity relationships of 8-(methylthio)- and 8-(acylthio)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines.
TBA
Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones.
TBA
Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties.
TBA
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.
TBA
Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
TBA
Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
TBA
Opiate receptor interaction of compounds derived from or structurally related to fentanyl.
TBA
Preparation and analgesic properties of amino acid derivatives of (-)-5,9 alpha-diethyl-2'-hydroxybenzomorphan.
TBA
Synthesis and analgesic activity of some 5-(4-hydroxyphenyl)-2-azabicyclo[3.2.1]octanes.
TBA
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
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
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
Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Mercachem
'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
Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2.
Medical University Of Lodz
Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine.
TBA
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University Of Bath
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)
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
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
The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2.
Biological Research Center Of The Hungarian Academy Of Sciences
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
Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.
University Of Maryland
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
University Of Innsbruck And Center For Molecular Biosciences Innsbruck-Cmbi
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute Of Montreal
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
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
Universit£T Des Saarlandes
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
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
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
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
University Of Cagliari
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 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
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
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
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
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.
University Of Lausanne
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
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.
Clinical Research Institute Of Montr£Al
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
University Of Maryland
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.
University Of Catania
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
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Southern Research Institute
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
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
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
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
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
Clinical Research Institute Of Montreal
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.
University Of Minnesota
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.
University Of Arizona
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
University Of Arizona
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
Clinical Research Institute Of Montreal
Systemic analgesic activity and delta-opioid selectivity in [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin.
Searle Research And Development
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
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
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
Universit£
[D-Pen2,D-Pen5]enkephalin analogues with increased affinity and selectivity for delta opioid receptors.
University Of Arizona
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
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
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
Istituto Superiore Di Sanit£
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
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
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.
R. W. Johnson Pharmaceutical Research Institute
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
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.
University Of Maryland
The LMC delta opioid recognition pharmacophore: comparison of SNC80 and oxymorphindole.
National Institute Of Diabetes
Delta opioid binding selectivity of 3-ether analogs of naltrindole.
National Institute Of Diabetes
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.
National Institute Of Diabetes
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
EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists
TBA
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
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
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
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
Hungarian Academy Of Sciences
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
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
University Of Cagliari
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
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
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
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
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
University Of Cagliari
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
Stereoselective synthesis and evaluation of all stereoisomers of Z4349, a novel and selective μ-opioid analgesic
TBA
Specific affinity labeling of μ opioid receptors in rat brain by S-activated sulfhydryldihydromorphine 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
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
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.
Vrije Universiteit Brussel
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
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
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
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
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
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
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
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
New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Kobe Gakuin University
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
University Of Catania
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
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Johnson & Johnson Pharmaceutical Research & Development
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
Kobe Gakuin 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
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Biological Research Center Of The Hungarian Academy Of Sciences
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.
Kobe Gakuin University
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
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
Crystal structures of dipeptides containing the Dmt-Tic pharmacophore.
National Institute Of Environmental Health Sciences
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.
Neurogen
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Tohoku Pharmaceutical University
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.
Niddk
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.
Lanzhou University
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.
Tohoku Pharmaceutical University
Dual Pharmacophores Explored via Structure-Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design.
TBA
Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.
National Institute Of Diabetes And Digestive And Kidney Diseases
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.
University Of Minnesota
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
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
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
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 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
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
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors.
Biological Research Centre Of The Hungarian Academy Of Sciences
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
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
Discovery of a Highly Selective and Potent ? Opioid Receptor Agonist from
Fudan University
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
Hungarian Academy Of Sciences
Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides.
University Of Ferrara
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Mayo Foundation
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
Eli Lilly
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.
TBA
Conformation of 2,9-dimethyl-3'-hydroxy-5-phenyl-6,7-genzomorphan and its relation to other analgetics and enkephalin.
TBA
Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone.
TBA
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
TBA
Paradoxical effects of N-cyanoalkyl substituents upon the activities of several classes of opioids.
TBA
Deoxymorphines: role of the phenolic hydroxyl in antinociception and opiate receptor interactions.
TBA
N-(2-Cyanoethyl) derivatives of meperidine, ketobemidone, and a potent 6,7-benzomorphan.
TBA
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
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid.
Oregon State University
Systematic replacement of amides by 1,4-disubstituted[1,2,3]triazoles in Leu-enkephalin and the impact on the delta opioid receptor activity.
Universit£
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£
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.
Clinical Research Institute Of Montreal
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.
Universit£
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
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
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
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
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.
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
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
Probes for narcotic receptor mediated phenomena. 15. (3S,4S)-(+)-trans-3-methylfentanyl isothiocyanate, a potent site-directed acylating agent for the delta opioid receptors in vitro.
National Institutes Of Health
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
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.
Merck Sharp & Dohme Research Laboratories
Development of novel LP1-based analogues with enhanced delta opioid receptor profile.
University Of Catania
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
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.
Clinical Research Institute Of Montreal
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
Delta opioid antagonist activity and binding studies of regioisomeric isothiocyanate derivatives of naltrindole: evidence for delta receptor subtypes.
University Of Minnesota
Conformationally restricted deltorphin analogues.
Clinical Research Institute Of Montreal
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.
Upjohn
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity.
University Of Arizona
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors.
National Institute Of Environmental Health Sciences
Symmetrical aryl linked bis-iminothiazolidinones as new chemical entities for the inhibition of monoamine oxidases: Synthesis, in vitro biological evaluation and molecular modelling analysis.
Quaid-I-Azam University
Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening.
Icahn School Of Medicine At Mount Sinai