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BindingDB contains 2.6M data for 1.1M Compounds and 8.9K Targets. Of those, 1,167K data for 538K Compounds and 4.4K Targets were curated by BindingDB curators.

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317 articles for thisTarget


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PMID
Data
Article Title
Organization
Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues.EBI
Medical University of Lodz
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/sEBI
University of Catania
Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge.EBI
Universit£ di Chieti-Pescara"G. d'Annunzio"
Assessment of the in vivo and in vitro opioid activity of bridged hexahydroaporphine and isoquinoline molecules.EBI
Creighton University
Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines.EBI
Anaquest Pharmaceuticals
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.EBI
University of Innsbruck
X-ray crystal structure of the opioid ligand naltrexonazine.EBI
TBA
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.EBI
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.EBI
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.EBI
TBA
3,7-Diazabicyclane: a new narcotic analgesic.EBI
TBA
Irreversible blockage of opioid receptor types by ester homologues of beta-funaltrexamine.EBI
TBA
Acylmorphinans. A novel class of potent analgesic agents.EBI
TBA
Opioid agonists and antagonists. 6-Desoxy-6-substituted lactone, epoxide, and glycidate ester derivatives of naltrexone and oxymorphone.EBI
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.EBI
TBA
Potential synthetic codeine substitutes: (-)-3-O-aryl-N-methylmorphinans.EBI
TBA
Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones.EBI
TBA
14 beta-(2-bromoacetamido)morphine and 14 beta-(2-bromoacetamido)morphinone.EBI
TBA
Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties.EBI
TBA
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.EBI
TBA
Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.EBI
TBA
Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.EBI
TBA
Opiate receptor interaction of compounds derived from or structurally related to fentanyl.EBI
TBA
Preparation and analgesic properties of amino acid derivatives of (-)-5,9 alpha-diethyl-2'-hydroxybenzomorphan.EBI
TBA
Synthesis and analgesic activity of some 5-(4-hydroxyphenyl)-2-azabicyclo[3.2.1]octanes.EBI
TBA
Some spiro analogues of the potent analgesic ketobemidone.EBI
TBA
Novel analogues of enkephalin: indentification of functional groups required for biological activity.EBI
TBA
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds.EBI
Mossakowski Medical Research Centre Polish Academy of Sciences
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.EBI
Clinical Research Institute of Montreal
[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.EBI
Nanjing Medical University
Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacyµ-Opioid Receptor (MOR)/d-Opioid Receptor (DOR) Ligands.EBI
University of Michigan
Evaluation of N-substituent structural variations in opioid receptor profile of LP1.EBI
University of Catania
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.EBI
Vrije Universiteit Brussel
Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.EBI
University of Michigan
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.EBI
Medical University of Lodz
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.EBI
Medical University of Lodz
Multitarget opioid ligands in pain relief: New players in an old game.EBI
University of Catania
Potentµ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.EBI
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.EBI
University of Michigan
Conformationally restrictedż-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.EBI
Mercachem
'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode.EBI
Clinical Research Institute of Montreal
Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities atµ (MOR),d (DOR), andż (KOR) Opioid Receptors.EBI
Torrey Pines Institute for Molecular Studies
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.EBI
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.EBI
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.EBI
Zhejiang University
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.EBI
Vrije Universiteit Brussel
Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2.EBI
Medical University of Lodz
Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine.EBI
TBA
Novel cyclic biphalin analogue with improved antinociceptive properties.EBI
Universit£ di Chieti-Pescara"G. d'Annunzio"
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.EBI
University of Bath
In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated DmtEBI
Vrije Universiteit Brussel
Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity.EBI
Nanjing Medical University
[Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/ż opioid activity profile.EBI
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.EBI
University of Michigan
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.EBI
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.EBI
Universit£ di Chieti-Pescara"G. d'Annunzio"
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacyµ opioid receptor (MOR) agonist/d opioid receptor (DOR) antagonist ligands.EBI
University of Michigan
Opioid receptor interactions and conformations of the 6 alpha and 6 beta epimers of oxymorphamine. Solid-state conformation of 6 alpha-oxymorphamine.EBI
TBA
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.EBI
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.EBI
Vrije Universiteit Brussel
The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2.EBI
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).EBI
Janssen Research and Development LLC
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties.EBI
Vrije Universiteit Brussel
Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.EBI
University of Maryland
Evaluation of N-substitution in 6,7-benzomorphan compounds.EBI
University of Catania
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.EBI
University of Innsbruck and Center for Molecular Biosciences Innsbruck-CMBI
"Carba"-analogues of fentanyl are opioid receptor agonists.EBI
Clinical Research Institute of Montreal
Synthesis and opioid receptor activity of indolopropellanes.EBI
Chinese Academy of Sciences
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.EBI
Kitasato University
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?EBI
Universit£t des Saarlandes
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.EBI
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.EBI
Stanford University School of Medicine
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).EBI
University of Ferrara
Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.EBI
Biological Research Center of the Hungarian Academy of Sciences
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.EBI
University of Maryland
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.EBI
Kyushu University
Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity.EBI
Taisho Pharmaceutical Co., Ltd
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.EBI
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.EBI
Sapienza University of Rome
Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.EBI
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].EBI
Southern Research Institute
Importance of phenolic address groups in opioid kappa receptor selective antagonists.EBI
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.EBI
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.EBI
GlaxoSmithKline
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.EBI
University of Arizona
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.EBI
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.EBI
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.EBI
University of Cagliary
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.EBI
University of Cagliari
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.EBI
University of Innsbruck
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.EBI
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.EBI
Research Triangle Institute
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.EBI
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.EBI
Research Triangle Institute
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.EBI
Clinical Research Institute of Montr£al
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.EBI
University of Maryland
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.EBI
University of Catania
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.EBI
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.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.EBI
Southern Research Institute
3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy.EBI
University of Bristol
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.EBI
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 rEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.EBI
University of Arizona
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.EBI
University of Ferrara
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.EBI
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.EBI
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.EBI
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.EBI
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.EBI
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.EBI
Clinical Research Institute of Montreal
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.EBI
University of Minnesota
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.EBI
University of Arizona
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.EBI
University of Arizona
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.EBI
Clinical Research Institute of Montreal
Systemic analgesic activity and delta-opioid selectivity in [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin.EBI
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.EBI
G.D. Searle and Co.
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-iodoEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Topographically designed analogues of [D-Pen,D-Pen5]enkephalin.EBI
University of Arizona
Synthesis and structure-activity relationships of deltorphin analogues.EBI
University of Ferrara
Function of negative charge in the"address domain" of deltorphins.EBI
National Institute of Environmental Health Sciences
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.EBI
Universit£ Louis Pasteur
[D-Pen2,D-Pen5]enkephalin analogues with increased affinity and selectivity for delta opioid receptors.EBI
University of Arizona
Synthesis of highly mu and delta opioid receptor selective peptides containing a photoaffinity group.EBI
University of Arizona
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.EBI
Smith Kline and French Laboratories
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.EBI
University of Paris
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.EBI
SRI International
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.EBI
Istituto Superiore di Sanit£
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.EBI
TBA
Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.EBI
TBA
Hybromet: a ligand for purifying opioid receptors.EBI
TBA
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.EBI
TBA
Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for mu or delta opiate receptors.EBI
TBA
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.EBI
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.EBI
National Institutes of Environmental Health Sciences
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.EBI
Southern Research Institute
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.EBI
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.EBI
F. Hoffmann-La Roche Inc
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.EBI
University of Maryland
The LMC delta opioid recognition pharmacophore: comparison of SNC80 and oxymorphindole.EBI
National Institute of Diabetes
Delta opioid binding selectivity of 3-ether analogs of naltrindole.EBI
National Institute of Diabetes
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.EBI
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.EBI
Institute for Bioorganic Research
 
Synthesis and biological evaluation of 14-alkoxymorphinans. 14.1 14-ethoxy-5-methyl substituted indolomorphinans with opioid receptor selectivityEBI
TBA
 
EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonistsEBI
TBA
Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists.EBI
Kitasato University
Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs.EBI
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.EBI
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.EBI
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.EBI
Vrije Universiteit Brussel
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.EBI
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.EBI
University of Innsbruck
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.EBI
University of Cagliari
Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans.EBI
University of Debrecen
Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.EBI
Vrije Universiteit Brussel
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).EBI
University of Pavia
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.EBI
Fudan University
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.EBI
The University of Kansas
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).EBI
Clinical Research Institute of Montreal
Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.EBI
University of Michigan
Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands.EBI
Institute for Molecular Studies
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.EBI
University of Cagliari
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.EBI
Universit£ di Roma
Akuammine and Dihydroakuammine, Two Indolomonoterpene Alkaloids Displaying Affinity for Opioid ReceptorsEBI
TBA
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by alpha-aminoxy acids.EBI
TBA
 
Stereoselective synthesis and evaluation of all stereoisomers of Z4349, a novel and selective μ-opioid analgesicEBI
TBA
 
Specific affinity labeling of μ opioid receptors in rat brain by S-activated sulfhydryldihydromorphine analogsEBI
TBA
 
Synthesis and biological properties of quaternized N-methylation analogs of D-Arg-2-dermorphin tetrapeptideEBI
TBA
 
A new approach to enhance bioavailability of biologically active peptides: conjugation of a δ opioid agonist to β-cyclodextrinEBI
TBA
 
Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin IEBI
TBA
 
New potent enkephalin analogs containing trifluoromethylamino acid residuesEBI
TBA
 
Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ1EBI
TBA
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.EBI
Medical University of Lodz
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.EBI
Vrije Universiteit Brussel
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].EBI
National University of Singapore
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.EBI
University of Cagliari
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.EBI
Hungarian Academy of Sciences
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.EBI
Lanzhou University
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.EBI
University of Queensland
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.EBI
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.EBI
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.EBI
Kobe Gakuin University
Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore.EBI
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.EBI
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).EBI
Medical University
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.EBI
Taisho Pharmaceutical Co., Ltd
Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.EBI
Hungarian Academy of Sciences
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.EBI
Lanzhou University
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.EBI
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.EBI
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.EBI
National University of Singapore
6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.EBI
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.EBI
Lanzhou University
Identification of potent phenyl imidazoles as opioid receptor agonists.EBI
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).EBI
University of Cagliari
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.EBI
Kobe Gakuin University
New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.EBI
Kobe Gakuin University
A new structural motif for mu-opioid antagonists.EBI
Vrije Universiteit Brussel
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.EBI
University of Catania
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.EBI
Kobe Gakuin University
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.EBI
University of Cagliary
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.EBI
Johnson & Johnson Pharmaceutical Research & Development
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.EBI
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.EBI
University of Innsbruck
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.EBI
Biological Research Center of the Hungarian Academy of Sciences
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.EBI
Kobe Gakuin University
Mechanism of action of the diazabicyclononanone-type kappa-agonists.EBI
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.EBI
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.EBI
Tohoku Pharmaceutical University
Crystal structures of dipeptides containing the Dmt-Tic pharmacophore.EBI
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.EBI
Neurogen Corporation
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.EBI
Tohoku Pharmaceutical University
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.EBI
NIDDK
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.EBI
Lanzhou University
Novel EBI
University of Catania
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.EBI
Tohoku Pharmaceutical University
Benzimidazolone-based selective ?EBI
University of Florida
Dual Pharmacophores Explored via Structure-Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design.EBI
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.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.EBI
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.EBI
Research Triangle Institute
Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.EBI
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.EBI
Istituto di Chimica Farmaceutica e Tossicologica
Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.EBI
Hungarian Academy of Sciences
Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.EBI
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.EBI
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.EBI
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.EBI
Clinical Research Institute of Montreal
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.EBI
Universit£t M£nster
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic ?-Opioid Receptor (MOR) Agonist/?-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.EBI
University of Michigan
Development of Novel Quinoxaline-Based ?-Opioid Receptor Agonists for the Treatment of Neuroinflammation.EBI
Universit£t M£nster
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.EBI
Research Triangle Institute
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors.EBI
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.EBI
The University of Arizona
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.EBI
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.EBI
Research Triangle Institute
(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist.EBI
University of Catania
Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.EBI
Eisai Co., Ltd.
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.EBI
Oregon State University
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.EBI
National Institute of Environmental Health Sciences
Discovery of a Highly Selective and Potent ? Opioid Receptor Agonist from EBI
Fudan University
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.EBI
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.EBI
University of Ferrara
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.EBI
Mayo Foundation
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.EBI
Eli Lilly and Company
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.EBI
TBA
Conformation of 2,9-dimethyl-3'-hydroxy-5-phenyl-6,7-genzomorphan and its relation to other analgetics and enkephalin.EBI
TBA
Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone.EBI
TBA
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.EBI
TBA
Paradoxical effects of N-cyanoalkyl substituents upon the activities of several classes of opioids.EBI
TBA
Deoxymorphines: role of the phenolic hydroxyl in antinociception and opiate receptor interactions.EBI
TBA
N-(2-Cyanoethyl) derivatives of meperidine, ketobemidone, and a potent 6,7-benzomorphan.EBI
TBA
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.EBI
University of Arizona
Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors.EBI
University of Ferrara
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI
Solvay Duphar B.V.
Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity ? opioid receptor (MOR) agonist/? opioid receptor (DOR) antagonist ligands.EBI
University of Michigan
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid.EBI
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.EBI
Universit£ de Sherbrooke
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.EBI
Eli Lilly and Company
Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation.EBI
Universit£ degli Studi "G. d'Annunzio" di Chieti-Pescara
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.EBI
Clinical Research Institute of Montreal
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.EBI
Universit£ Montpellier 1
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.EBI
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.EBI
Searle
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 1. Conformational constraint in the"message" sequence.EBI
Oregon State University
Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties.EBI
Tohoku College of Pharmacy
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.EBI
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.EBI
TBA
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.EBI
University of Bath
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.EBI
TBA
Selective kappa opioid antagonists for treatment of addiction, are we there yet?EBI
University of Science and Technology
7?-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues.EBI
Fudan University
Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile.EBI
Universit£ di Chieti-Pescara "G. d'Annunzio"
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl).EBI
University of Kansas
Original endomorphin-1 analogues exhibit good analgesic effects.EBI
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.EBI
University of Arizona
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.EBI
TBA
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.EBI
UA 498 CNRS
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic ? Receptor Ligands with Exocyclic Amino Moiety.EBI
Universit£t M£nster
Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position.EBI
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.EBI
National Institutes of Health
Dermorphin analogues carrying an increased positive net charge in their"message" domain display extremely high mu opioid receptor selectivity.EBI
Clinical Research Institute of Montreal
?-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.EBI
Vrije Universiteit Brussel
Chemical space screening around PheEBI
Vrije Universiteit Brussel
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.EBI
Merck Sharp & Dohme Research Laboratories
Development of novel LP1-based analogues with enhanced delta opioid receptor profile.EBI
University of Catania
Original endomorphin-1 analogues exhibit good analgesic effects with minimal implications for human sperm motility.EBI
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.EBI
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.EBI
Hebrew University of Jerusalem
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.EBI
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.EBI
Oregon State University
Preparation and opioid activity of analogues of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide.EBI
G.D. Searle and Co.
Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites.EBI
University of Ferrara
Delta opioid antagonist activity and binding studies of regioisomeric isothiocyanate derivatives of naltrindole: evidence for delta receptor subtypes.EBI
University of Minnesota
Conformationally restricted deltorphin analogues.EBI
Clinical Research Institute of Montreal
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.EBI
Upjohn Company
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity.EBI
University of Arizona
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors.EBI
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.BDB
Quaid-i-Azam University
Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening.BDB
Icahn School of Medicine at Mount Sinai
Novel 4-heteroaryl-antipyrines as DPP-IV inhibitors.BDB
Cairo University
Characterisation of melanocortin receptor subtypes by radioligand binding analysis.BDB
Uppsala