The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28318942 |
10 |
Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues. |
Medical University of Lodz |
| 27721146 |
22 |
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s |
University of Catania |
| 28435535 |
8 |
Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge. |
Universit£ |
| 28105278 |
10 |
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds. |
Mossakowski Medical Research Centre Polish Academy of Sciences |
| 27676089 |
35 |
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists. |
Clinical Research Institute of Montreal |
| 27301366 |
30 |
[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1. |
Nanjing Medical University |
| 27148755 |
75 |
Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacyµ-Opioid Receptor (MOR)/d-Opioid Receptor (DOR) Ligands. |
University of Michigan |
| 27234885 |
31 |
Evaluation of N-substituent structural variations in opioid receptor profile of LP1. |
University of Catania |
| 26713106 |
59 |
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics. |
Vrije Universiteit Brussel |
| 26713104 |
24 |
Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics. |
University of Michigan |
| 26944625 |
26 |
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs. |
Medical University of Lodz |
| 26785295 |
35 |
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration. |
Medical University of Lodz |
| 26656913 |
85 |
Multitarget opioid ligands in pain relief: New players in an old game. |
University of Catania |
| 26789491 |
44 |
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 |
| 26712115 |
36 |
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 |
| 26524472 |
75 |
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 |
| 26491810 |
35 |
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin. |
The University of Kansas |
| 26330078 |
51 |
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists. |
Harvard Medical School |
| 26323872 |
49 |
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives. |
University of Arizona |
| 26316468 |
53 |
Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors. |
University of Arizona |
| 26299827 |
43 |
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands. |
University of Arizona |
| 26125201 |
62 |
Structural Requirements for CNS Active Opioid Glycopeptides. |
The University of Arizona |
| 25168746 |
28 |
Synthesis and analgesic activity of alkylated, reduced and constrained oligoheterocyclic peptidomimetic analogs of Leu-enkephalin. |
University of Monastir |
| 25129170 |
20 |
'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode. |
Clinical Research Institute of Montreal |
| 25996309 |
49 |
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 |
| 26005537 |
72 |
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
Medical University of Lodz |
| 25898137 |
61 |
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 |
| 25559207 |
92 |
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 |
| 25544687 |
60 |
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics. |
Vrije Universiteit Brussel |
| 25087049 |
56 |
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 |
| 25047937 |
9 |
Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
Medical University of Lodz |
| 25456075 |
16 |
Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine. |
TBA |
| 25221662 |
24 |
Novel cyclic biphalin analogue with improved antinociceptive properties. |
Universit£ |
| 24761755 |
76 |
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity. |
University of Bath |
| 24839540 |
26 |
In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt |
Vrije Universiteit Brussel |
| 24613457 |
64 |
Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity. |
Nanjing Medical University |
| 24602401 |
40 |
[Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/¿ opioid activity profile. |
Nanjing Medical University |
| 24641190 |
16 |
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 |
| 15743203 |
272 |
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) |
| 23438330 |
174 |
Orvinols with mixed kappa/mu opioid receptor agonist activity. |
University of Bath |
| 23547584 |
19 |
Biological active analogues of the opioid peptide biphalin: mixeda/ß(3)-peptides. |
Universit£ |
| 23419026 |
40 |
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacyµ opioid receptor (MOR) agonist/d opioid receptor (DOR) antagonist ligands. |
University of Michigan |
| 23360448 |
18 |
Development of¿ opioid receptor antagonists. |
Research Triangle Institute |
| 22325949 |
28 |
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 |
| 23102273 |
60 |
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution. |
Vrije Universiteit Brussel |
| 22957923 |
20 |
The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2. |
Biological Research Center of The Hungarian Academy of Sciences |
| 22695132 |
56 |
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 |
| 21978284 |
42 |
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties. |
Vrije Universiteit Brussel |
| 22677527 |
38 |
Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors. |
University of Maryland |
| 22394120 |
7 |
The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues. |
Universit£ |
| 21128594 |
93 |
Development of potent µ and d opioid agonists with high lipophilicity. |
University of Arizona |
| 20599386 |
46 |
Evaluation of N-substitution in 6,7-benzomorphan compounds. |
University of Catania |
| 20580236 |
60 |
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors. |
University of Innsbruck and Center For Molecular Biosciences Innsbruck-Cmbi |
| 20547453 |
122 |
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain. |
University of Arizona |
| 20218625 |
27 |
"Carba"-analogues of fentanyl are opioid receptor agonists. |
Clinical Research Institute of Montreal |
| 20560643 |
71 |
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists. |
University of Arizona |
| 19362480 |
22 |
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. |
Kitasato University |
| 19211245 |
27 |
Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A. |
Harvard Medical School |
| 18403056 |
8 |
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
Universit£T Des Saarlandes |
| 18370374 |
12 |
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility. |
Vrije Universiteit Brussel |
| 18311909 |
10 |
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 |
| 18178091 |
24 |
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502). |
University of Ferrara |
| 18166466 |
12 |
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors. |
Harvard Medical School |
| 17981041 |
79 |
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers. |
Mclean Hospital |
| 18293909 |
5 |
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor. |
University of Minnesota |
| 18062664 |
13 |
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 |
| 17659872 |
15 |
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands. |
University of Maryland |
| 17395470 |
40 |
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2. |
Kyushu University |
| 17267226 |
46 |
Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity. |
Taisho Pharmaceutical |
| 16814543 |
14 |
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 |
| 16942034 |
19 |
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore. |
University of Cagliari |
| 16509592 |
101 |
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 |
| 16250647 |
71 |
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£ |
| 15857143 |
48 |
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 |
| 16033285 |
24 |
Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency. |
University of Innsbruck |
| 15456262 |
32 |
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£ |
| 14998329 |
142 |
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 |
| 14761209 |
15 |
Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
Research Triangle Institute |
| 12699394 |
30 |
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 |
| 12570383 |
46 |
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 |
| 12954070 |
24 |
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic. |
University of Innsbruck |
| 12825951 |
54 |
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 |
| 11806723 |
20 |
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 |
| 12459023 |
46 |
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore. |
University of Cagliari |
| 12431065 |
72 |
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
University of Innsbruck |
| 12139463 |
24 |
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
Research Triangle Institute |
| 12036366 |
12 |
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
Universit£ |
| 11311071 |
53 |
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 |
| 11300879 |
77 |
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 |
| 11300867 |
32 |
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 |
| 11689075 |
20 |
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation. |
University of Lausanne |
| 11495579 |
24 |
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 |
| 11405645 |
13 |
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 |
| 10691681 |
17 |
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors. |
Clinical Research Institute of Montr£Al |
| 10956208 |
121 |
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
University of Catania |
| 10229636 |
30 |
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
National Institute of Diabetes |
| 10639287 |
62 |
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 |
| 10543877 |
25 |
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides. |
Uppsala University |
| 10479286 |
53 |
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
Southern Research Institute |
| 9857087 |
63 |
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile. |
Vrije Universiteit Brussel |
| 9836606 |
12 |
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
University of Minnesota |
| 9804688 |
51 |
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 |
| 9719602 |
24 |
3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy. |
University of Bristol |
| 9667975 |
86 |
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
Southern Research Institute |
| 9057856 |
53 |
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 |
| 9397176 |
28 |
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors. |
University of Arizona |
| 9301674 |
60 |
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity. |
University of Ferrara |
| 9288177 |
20 |
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. |
University of Ferrara |
| 9288176 |
95 |
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 |
| 8642567 |
64 |
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 |
| 7739013 |
26 |
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 |
| 7739011 |
90 |
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 |
| 8164255 |
23 |
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects. |
Clinical Research Institute of Montreal |
| 7932569 |
116 |
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 |
| 8064796 |
10 |
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library. |
Chiron |
| 8035418 |
30 |
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 |
| 8201592 |
27 |
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity. |
University of Arizona |
| 8289188 |
30 |
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors. |
University of Arizona |
| 8230106 |
16 |
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
Clinical Research Institute of Montreal |
| 8393489 |
25 |
A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines. |
Glaxo Group Research |
| 8390575 |
28 |
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
Universit£ |
| 1311764 |
4 |
Systemic analgesic activity and delta-opioid selectivity in [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin. |
Searle Research and Development |
| 1323677 |
18 |
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 |
| 1322988 |
60 |
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 |
| 1322987 |
34 |
Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at sigma, PCP, and mu opioid receptors. |
Research Triangle Institute |
| 1648137 |
30 |
Topographically designed analogues of [D-Pen,D-Pen5]enkephalin. |
University of Arizona |
| 1851843 |
96 |
Synthesis and structure-activity relationships of deltorphin analogues. |
University of Ferrara |
| 1849997 |
42 |
Function of negative charge in the"address domain" of deltorphins. |
National Institute of Environmental Health Sciences |
| 2167979 |
43 |
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor. |
Universit£ |
| 2153205 |
10 |
[D-Pen2,D-Pen5]enkephalin analogues with increased affinity and selectivity for delta opioid receptors. |
University of Arizona |
| 2537426 |
12 |
Synthesis of highly mu and delta opioid receptor selective peptides containing a photoaffinity group. |
University of Arizona |
| 2536436 |
24 |
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5. |
Smith Kline and French Laboratories |
| 2831363 |
19 |
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines. |
Eli Lilly |
| 2828622 |
71 |
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides. |
University of Paris |
| 2845084 |
22 |
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities. |
Sri International |
| 3033248 |
3 |
Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists. |
TBA |
| 3007760 |
93 |
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
TBA |
| 2878079 |
22 |
Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors. |
TBA |
| 2999408 |
11 |
Hybromet: a ligand for purifying opioid receptors. |
TBA |
| 2999401 |
20 |
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers. |
TBA |
| 6150112 |
24 |
Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for mu or delta opiate receptors. |
TBA |
| 6296388 |
68 |
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity. |
TBA |
| 15115401 |
24 |
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 |
| 12643945 |
36 |
Structure-activity relationships of some opiate glycosides. |
Ultrafine Ufc |
| 12565965 |
45 |
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
Southern Research Institute |
| 11425550 |
62 |
Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor. |
R. W. Johnson Pharmaceutical Research Institute |
| 10782696 |
67 |
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 |
| 11133084 |
14 |
Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids. |
Universit£ |
| 11078198 |
12 |
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
University of Maryland |
| 10866377 |
9 |
Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity. |
Universit£ |
| 10340622 |
47 |
Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin. |
Organon Laboratories |
| 10617086 |
21 |
Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
National Institute of Diabetes |
| 10612597 |
31 |
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 |
| 10571174 |
25 |
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor. |
Research Triangle Institute |
| 9871544 |
24 |
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives. |
National Institute of Diabetes |
| 9873603 |
23 |
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models. |
University of Michigan |
| 9873480 |
35 |
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 |
| | 17 |
Synthesis and biological evaluation of 14-alkoxymorphinans. 14.1 14-ethoxy-5-methyl substituted indolomorphinans with opioid receptor selectivity |
TBA |
| | 51 |
EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists |
TBA |
| 22204910 |
17 |
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues. |
Harvard Medical School |
| 22197670 |
51 |
Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists. |
Kitasato University |
| 22047797 |
16 |
Effect of 2',6'-dimethyl-L-tyrosine (Dmt) on pharmacological activity of cyclic endomorphin-2 and morphiceptin analogs. |
Medical University of Lodz |
| 21925887 |
10 |
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands. |
University of Arizona |
| 21870874 |
30 |
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 |
| 21864951 |
6 |
Derivatives of pyrrolo[3,4-d]pyridazinone, a new class of analgesic agents. |
Wroclaw Medical University |
| 21413804 |
21 |
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 |
| 21366266 |
66 |
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 |
| 21287991 |
43 |
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
Hungarian Academy of Sciences |
| 21235243 |
35 |
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 |
| 20692738 |
34 |
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. |
Sapienza University of Rome |
| 20637637 |
46 |
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds. |
University of Cagliari |
| 20617791 |
70 |
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. |
University of Arizona |
| 20476738 |
14 |
Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues. |
Universit£ |
| 20413312 |
17 |
Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans. |
University of Debrecen |
| 20137938 |
28 |
Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds. |
Vrije Universiteit Brussel |
| 19932964 |
26 |
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton. |
Fudan University |
| 19762245 |
69 |
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 |
| 19640720 |
4 |
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 |
| 19621878 |
19 |
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. |
The University of Kansas |
| 19827750 |
39 |
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1). |
Clinical Research Institute of Montreal |
| 19807094 |
45 |
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues. |
University of Kansas |
| 19788201 |
32 |
Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties. |
University of Michigan |
| 19576786 |
129 |
Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands. |
Institute For Molecular Studies |
| 19715279 |
20 |
Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis. |
The University of Kansas |
| 19642675 |
60 |
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore. |
University of Cagliari |
| 19560919 |
28 |
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. |
Universit£ |
| 1317407 |
7 |
Akuammine and Dihydroakuammine, Two Indolomonoterpene Alkaloids Displaying Affinity for Opioid Receptors |
TBA |
| 15984054 |
21 |
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by alpha-aminoxy acids. |
TBA |
| | 17 |
trans N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonists |
TBA |
| | 35 |
Stereoselective synthesis and evaluation of all stereoisomers of Z4349, a novel and selective μ-opioid analgesic |
TBA |
| | 8 |
Specific affinity labeling of μ opioid receptors in rat brain by S-activated sulfhydryldihydromorphine analogs |
TBA |
| | 16 |
Synthesis and biological properties of quaternized N-methylation analogs of D-Arg-2-dermorphin tetrapeptide |
TBA |
| | 4 |
A new approach to enhance bioavailability of biologically active peptides: conjugation of a δ opioid agonist to β-cyclodextrin |
TBA |
| | 38 |
The use of synthetic peptide combinatorial libraries for the determination of peptide ligands in radio-receptor assays: Opioid peptides |
TBA |
| | 8 |
Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin I |
TBA |
| | 6 |
New potent enkephalin analogs containing trifluoromethylamino acid residues |
TBA |
| | 4 |
Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ1 |
TBA |
| 19435668 |
20 |
Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2. |
Medical University of Lodz |
| 19253970 |
39 |
Mixed kappa/mu opioid receptor agonists: the 6 beta-naltrexamines. |
University of Bath |
| 19147366 |
60 |
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor. |
Mclean Hospital |
| 19062273 |
41 |
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold. |
Vrije Universiteit Brussel |
| 18821747 |
45 |
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 |
| 18800771 |
26 |
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp]. |
National University of Singapore |
| 18680274 |
44 |
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic. |
University of Cagliari |
| 18572932 |
64 |
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
Hungarian Academy of Sciences |
| 18490168 |
32 |
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. |
Lanzhou University |
| 18468445 |
26 |
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
University of Queensland |
| 18207400 |
17 |
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
Medical University of Lodz |
| 17851080 |
6 |
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 |
| 17497839 |
72 |
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 |
| 17339114 |
27 |
Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore. |
University of Cagliari |
| 17329100 |
34 |
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors. |
University of Arizona |
| 17315860 |
40 |
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 |
| 17266203 |
29 |
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 |
| 17234422 |
118 |
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor. |
Taisho Pharmaceutical |
| 17228874 |
18 |
Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists. |
Hungarian Academy of Sciences |
| 17201419 |
93 |
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. |
University of Arizona |
| 17188879 |
16 |
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization. |
Lanzhou University |
| 17142049 |
40 |
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
Kobe Gakuin University |
| 16949282 |
12 |
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 |
| 16913729 |
9 |
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 |
| 16828552 |
20 |
Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity. |
University of Arizona |
| 16759107 |
18 |
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 |
| 16750366 |
104 |
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 |
| 16682191 |
21 |
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 |
| 16483774 |
66 |
Identification of potent phenyl imidazoles as opioid receptor agonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 16366592 |
33 |
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 |
| 16335927 |
48 |
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists. |
Kobe Gakuin University |
| 16275086 |
18 |
Synthesis and biological activity of the first cyclic biphalin analogues. |
University of Arizona |
| 16183273 |
12 |
New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif. |
Kobe Gakuin University |
| 15887972 |
8 |
A new structural motif for mu-opioid antagonists. |
Vrije Universiteit Brussel |
| 15863298 |
20 |
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides. |
University of Catania |
| 15857130 |
37 |
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models. |
University of Szeged |
| 15857121 |
1 |
Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor. |
Università |
| 15658871 |
28 |
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2. |
Kobe Gakuin University |
| 15588089 |
10 |
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic. |
University of Cagliary |
| 15456245 |
44 |
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders. |
Johnson & Johnson Pharmaceutical Research & Development |
| 15214786 |
64 |
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties. |
Kobe Gakuin University |
| 15163203 |
45 |
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 |
| 14736254 |
70 |
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
Biological Research Center of The Hungarian Academy of Sciences |
| 14711314 |
63 |
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 |
| 12954053 |
39 |
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2. |
University of Maryland |
| 12852751 |
34 |
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia. |
Kobe Gakuin University |
| 12672238 |
3 |
Mechanism of action of the diazabicyclononanone-type kappa-agonists. |
UniversitäT WüRzburg |
| 12657261 |
32 |
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 |
| 12459018 |
6 |
Crystal structures of dipeptides containing the Dmt-Tic pharmacophore. |
National Institute of Environmental Health Sciences |
| 12372527 |
27 |
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin. |
Institute For Molecular Studies |
| 12190304 |
10 |
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 |
| 11958984 |
24 |
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity. |
Tohoku Pharmaceutical University |
| 11755345 |
45 |
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives. |
Niddk |
| 32199689 |
64 |
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
Lanzhou University |
| 32435370 |
45 |
Novel |
University of Catania |
| 11212102 |
24 |
Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4. |
Tohoku Pharmaceutical University |
| 11150176 |
9 |
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 |
| 30916966 |
116 |
Dual Pharmacophores Explored via Structure-Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design. |
TBA |
| 10893314 |
24 |
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
University of Minnesota |
| 10866400 |
18 |
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 |
| 10843229 |
92 |
Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists. |
R. W. Johnson Pharmaceutical Research Institute |
| 10841790 |
24 |
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 |
| 10741545 |
36 |
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands. |
Pfizer |
| 10691683 |
22 |
Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays. |
University of Arizona |
| 10639279 |
26 |
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 |
| 10585210 |
60 |
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 |
| 10479285 |
17 |
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 |
| 10340623 |
31 |
Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis. |
Organon Laboratories |
| 30924650 |
73 |
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic ?-Opioid Receptor (MOR) Agonist/?-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability. |
University of Michigan |
| 9873693 |
24 |
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists. |
Research Triangle Institute |
| 31220675 |
88 |
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. |
Biological Research Centre of The Hungarian Academy of Sciences |
| 9822547 |
41 |
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor. |
The University of Arizona |
| 9767649 |
24 |
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists. |
Research Triangle Institute |
| 9599247 |
57 |
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 |
| 30822708 |
24 |
(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist. |
University of Catania |
| 31498617 |
29 |
Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists. |
Eisai |
| 9288174 |
24 |
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as antagonists of the NMDA receptor-channel complex. |
Boehringer Ingelheim Pharmaceuticals |
| 9276018 |
47 |
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution. |
Oregon State University |
| 9258365 |
28 |
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues. |
National Institute of Environmental Health Sciences |
| 31738550 |
78 |
Discovery of a Highly Selective and Potent ? Opioid Receptor Agonist from |
Fudan University |
| 9083489 |
30 |
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3. |
Hungarian Academy of Sciences |
| 26611918 |
45 |
Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations. |
University of Arizona |
| 8576920 |
34 |
Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides. |
University of Ferrara |
| 8558529 |
195 |
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 |
| 26212775 |
77 |
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities. |
University of Arizona |
| 8410999 |
81 |
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
Eli Lilly |
| 8410998 |
129 |
Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors. |
Eli Lilly |
| 8355251 |
8 |
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 |
| 8289187 |
47 |
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. |
University of Arizona |
| 8254604 |
50 |
Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. |
University of Ferrara |
| 8246239 |
84 |
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives. |
Solvay Duphar |
| 24365161 |
45 |
Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity ? opioid receptor (MOR) agonist/? opioid receptor (DOR) antagonist ligands. |
University of Michigan |
| 24220171 |
5 |
Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration. |
Medical University of Lodz |
| 8097539 |
10 |
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid. |
Oregon State University |
| 8057274 |
18 |
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 |
| 23974016 |
26 |
Hybrid peptides endomorphin-2/DAMGO: design, synthesis and biological evaluation. |
Universit£ |
| 23932788 |
60 |
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile. |
Clinical Research Institute of Montreal |
| 24648867 |
58 |
Chiral Effect of a Phe Residue in Position 3 of the Dmt |
University of Arizona |
| 23822516 |
142 |
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations. |
Universit£ |
| 23768905 |
13 |
Synthesis and changes in affinity for NOP and opioid receptors of novel hexapeptides containing ?(2)-tryptophan analogues. |
Bulgarian Academy of Sciences |
| 7932540 |
38 |
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 |
| 7908696 |
45 |
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 |
| 23623418 |
140 |
Effect of anchoring 4-anilidopiperidines to opioid peptides. |
University of Arizona |
| 7608905 |
24 |
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 1. Conformational constraint in the"message" sequence. |
Oregon State University |
| 7562933 |
24 |
Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
Tohoku College of Pharmacy |
| 7490727 |
72 |
(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 |
| 15743210 |
16 |
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
University of Bath |
| 29107424 |
27 |
Selective kappa opioid antagonists for treatment of addiction, are we there yet? |
University of Science and Technology |
| 30054192 |
71 |
7?-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues. |
Fudan University |
| 28835802 |
12 |
Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile. |
Universit£ |
| 29273415 |
15 |
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl). |
University of Kansas |
| 28256374 |
10 |
Original endomorphin-1 analogues exhibit good analgesic effects. |
The First Hospital of Lanzhou University |
| 2903246 |
58 |
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 |
| 2876099 |
51 |
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties. |
TBA |
| 2845081 |
24 |
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors. |
Ua 498 Cnrs |
| 2822930 |
48 |
Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position. |
Clinical Research Institute of Montreal |
| 2563773 |
26 |
New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties. |
Boc Technical Center |
| 2537427 |
24 |
Dermorphin analogues carrying an increased positive net charge in their"message" domain display extremely high mu opioid receptor selectivity. |
Clinical Research Institute of Montreal |
| 29152051 |
40 |
?-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds. |
Vrije Universiteit Brussel |
| 29853330 |
106 |
Chemical space screening around Phe |
Vrije Universiteit Brussel |
| 2170652 |
25 |
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics. |
Anaquest Pharmaceuticals |
| 28734666 |
23 |
Development of novel LP1-based analogues with enhanced delta opioid receptor profile. |
University of Catania |
| 28377055 |
12 |
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 |
| 28314512 |
33 |
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 |
| 1714957 |
12 |
Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
Hebrew University of Jerusalem |
| 1671414 |
10 |
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds. |
Istituto Superiore Di Sanità |
| 1656045 |
26 |
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity. |
Clinical Research Institute of Montreal |
| 1360025 |
27 |
Effect of modification of the basic residues of dynorphin A-(1-13) amide on kappa opioid receptor selectivity and opioid activity. |
Oregon State University |
| 1346276 |
25 |
Preparation and opioid activity of analogues of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide. |
G.D. Searle And |
| 1335080 |
20 |
Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites. |
University of Ferrara |
| 1331451 |
68 |
Conformationally restricted deltorphin analogues. |
Clinical Research Institute of Montreal |
| 1320122 |
55 |
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity. |
University of Arizona |
| 1313878 |
36 |
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors. |
National Institute of Environmental Health Sciences |
| 27863747 |
21 |
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 |
| 27224444 |
14 |
Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. |
Broad Institute |
| 26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
| 27128978 |
8 |
Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening. |
Icahn School of Medicine At Mount Sinai |
| 26032047 |
15 |
Novel 4-heteroaryl-antipyrines as DPP-IV inhibitors. |
Cairo University |
| 25996453 |
4 |
Synthesis of novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene derivatives and their biological evaluation against protein tyrosine phosphatase 1B. |
Jiangnan University |
| 7774675 |
35 |
Characterisation of melanocortin receptor subtypes by radioligand binding analysis. |
Uppsala |
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