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 |
28218838 |
69 |
Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective¿-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. |
Dr. August Wolff Gmbh & Co. Kg Arzneimittel |
28011222 |
16 |
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands. |
West Virginia University School of Pharmacy |
27721146 |
22 |
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s |
University of Catania |
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 |
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 |
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 |
26411794 |
46 |
Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines. |
Mercachem |
25283554 |
43 |
Design, synthesis, and structure-activity relationship of novel opioid¿ receptor selective agonists:a-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton. |
Kitasato University |
25168746 |
28 |
Synthesis and analgesic activity of alkylated, reduced and constrained oligoheterocyclic peptidomimetic analogs of Leu-enkephalin. |
University of Monastir |
25147605 |
52 |
Synthesis and Pharmacology of a Novel¿ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton. |
Kitasato University |
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 |
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 |
25062506 |
102 |
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted¿-opioid receptor agonists. |
Westf£Lische Wilhelms-Universit£T M£Nster |
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 |
25248680 |
67 |
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies. |
Kitasato University |
24856182 |
23 |
Combination of cyclohexane and piperazine based¿-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines. |
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster |
24761755 |
76 |
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity. |
University of Bath |
24690494 |
92 |
Antagonists of the kappa opioid receptor. |
The Scripps Research Institute |
24900842 |
71 |
Novel delta opioid receptor agonists with oxazatricyclodecane structure. |
Kitasato University |
24602401 |
40 |
[Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/¿ opioid activity profile. |
Nanjing Medical University |
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 |
23360448 |
18 |
Development of¿ opioid receptor antagonists. |
Research Triangle Institute |
23200250 |
36 |
The effect of 17-N substituents on the activity of the opioid¿ receptor in nalfurafine derivatives. |
Kitasato University |
16290934 |
51 |
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1. |
Pfizer |
23131341 |
50 |
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 3: synthesis of novel triplet drugs with the bis(epoxymethano) or bis(dimethylepoxymethano) structure (double-capped triplet). |
Kitasato University |
23103094 |
39 |
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies. |
Kitasato University |
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 |
23134120 |
72 |
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist. |
University of Innsbruck |
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 |
23043264 |
20 |
Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversibleµ opioid receptor antagonist effects. |
University of Bristol |
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 |
22967810 |
102 |
Synthesis of quinolinomorphinan derivatives as highly selectived opioid receptor ligands. |
Kitasato University |
22742909 |
24 |
Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies. |
Kitasato University |
22583618 |
8 |
Kappa agonist CovX-Bodies. |
Pfizer |
22460026 |
39 |
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain. |
Kitasato University |
22445285 |
26 |
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies. |
Kitasato University |
21641798 |
16 |
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1. |
Kitasato University |
20931963 |
112 |
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome. |
Aska Pharmaceutical |
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 |
20441176 |
76 |
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives. |
Wilhelms-Universit£T M£Nster |
20218625 |
27 |
"Carba"-analogues of fentanyl are opioid receptor agonists. |
Clinical Research Institute of Montreal |
19962305 |
2 |
Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. |
Kitasato University |
19362480 |
22 |
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. |
Kitasato University |
19349178 |
4 |
Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction. |
Kitasato University |
19464172 |
74 |
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
Adolor |
19253983 |
37 |
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity. |
University of Bath |
18755589 |
2 |
Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction. |
Kitasato University |
19027293 |
149 |
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
Rensselaer Polytechnic Institute |
18990576 |
11 |
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology. |
Kitasato University |
18829333 |
28 |
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
Toray Industries |
18637671 |
21 |
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
Toray Industries |
18468907 |
64 |
Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis. |
Torrey Pines Institute For Molecular Studies |
18337104 |
7 |
Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies. |
Kitasato University |
17420073 |
31 |
Synthesis of bridged piperazines with sigma receptor affinity. |
Institut F£R Pharmazeutische Und Medizinische Chemie |
17402725 |
9 |
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors. |
University of Missouri-Columbia |
17004724 |
146 |
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring. |
University of Bristol |
16913723 |
78 |
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones. |
University of Bristol |
16777416 |
80 |
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. |
University of Kentucky |
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 |
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 |
12593647 |
49 |
2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists. |
Harvard University |
12930147 |
96 |
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
Universit£ |
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 |
12801235 |
5 |
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents. |
University of Vermont |
12723940 |
145 |
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
Research Triangle Institute |
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 |
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 |
11543672 |
24 |
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
Clinical Research Institute of Montreal |
11495592 |
12 |
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies. |
Pharmazeutisches Institut Der Universit£T Freiburg |
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 |
10794701 |
48 |
Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol. |
University of Bristol |
10753461 |
13 |
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function. |
University of Minnesota |
11000010 |
27 |
Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives. |
Rensselaer Polytechnic Institute |
10956208 |
121 |
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
University of Catania |
10841791 |
8 |
Modeling of kappa-opioid receptor/agonists interactions using pharmacophore-based and docking simulations. |
Universit£ |
10633042 |
30 |
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence. |
Harvard Medical School |
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 |
10479286 |
53 |
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
Southern Research Institute |
9857089 |
32 |
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
Research Triangle 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 |
9667975 |
86 |
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
Southern Research Institute |
9057861 |
33 |
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays. |
University of Washington |
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 |
8627605 |
10 |
Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide"address" recognition at kappa opioid receptors. |
University of Minnesota |
8648612 |
30 |
Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells. |
University of Minnesota |
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 |
7853350 |
33 |
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol. |
University of Washington |
7853332 |
27 |
7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
University of Minnesota |
7636870 |
18 |
Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime. |
University of Innsbruck |
8126697 |
30 |
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
University of Minnesota |
7996538 |
42 |
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol. |
University of Washington |
8071934 |
30 |
Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide. |
University of Washington |
8021929 |
13 |
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
University of Minnesota |
8182708 |
18 |
Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
University of Minnesota |
8394935 |
4 |
A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists. |
University of Minnesota |
8360887 |
9 |
Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. |
University of Minnesota |
8390575 |
28 |
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
Universit£ |
8380614 |
6 |
A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
University of Minnesota |
1315870 |
39 |
Substitution on the Phe3 aromatic ring in cyclic delta opioid receptor-selective dermorphin/deltorphin tetrapeptide analogues: electronic and lipophilic requirements for receptor affinity. |
University of Michigan |
1361580 |
25 |
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors. |
Oregon State University |
1335078 |
76 |
O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay. |
University of Washington |
1333014 |
12 |
Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, delta opioid receptor selective tetrapeptide (JOM-13) enhances delta receptor binding affinity and selectivity. |
University of Michigan |
1333013 |
29 |
Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
University of Minnesota |
1323679 |
21 |
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
Zambeletti Research Laboratories |
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 |
1320121 |
48 |
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol. |
University of Washington |
1319495 |
21 |
Selective reversible and irreversible ligands for the kappa opioid receptor. |
National Taiwan University |
1319493 |
31 |
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents. |
National Institute of Diabetes and Digestive and Kidney Diseases |
1648136 |
12 |
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
University of Minnesota |
1851846 |
23 |
Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
University of Minnesota |
1849995 |
12 |
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
University of Minnesota |
1659636 |
51 |
Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists. |
Ici Pharmaceuticals Group |
1846919 |
26 |
Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity. |
Parke-Davis Research Unit |
2167979 |
43 |
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor. |
Universit£ |
2160538 |
84 |
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
University of Minnesota |
2172538 |
58 |
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes. |
National Institute of Diabetes and Digestive and Kidney Diseases |
2153208 |
3 |
Highly selective kappa-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted-cyclohexyl]arylacetamide derivatives. |
Parke-Davis Research Unit |
2547074 |
16 |
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
National Institute of Digestive |
2542556 |
65 |
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides. |
Ciba-Geigy |
2832603 |
68 |
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives. |
Parke-Davis Research Unit |
2831363 |
19 |
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines. |
Eli Lilly |
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 |
2887656 |
48 |
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues. |
TBA |
2879914 |
30 |
Peptides as receptor selectivity modulators of opiate pharmacophores. |
TBA |
2409281 |
9 |
10-Ketonaltrexone and 10-ketooxymorphone. |
TBA |
12565965 |
45 |
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
Southern Research Institute |
11294396 |
57 |
Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole. |
University of Bristol |
11591513 |
87 |
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan. |
Harvard Medical School |
11425545 |
22 |
3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties. |
Pharmacia |
11055333 |
21 |
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
University of Bristol |
10673107 |
63 |
8-Aminocyclazocine analogues: synthesis and structure-activity relationships. |
Institute |
10340622 |
47 |
Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin. |
Organon Laboratories |
10206545 |
40 |
Ring constrained analogues of the orvinols: the furanomorphides. |
University of Bristol |
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 |
| 9 |
Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the -selective opioid receptor antagonist cyprodime |
TBA |
| 51 |
EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists |
TBA |
| 21 |
Neurotensin receptor binding and antinociceptive activity for lipophilic N-amido neurotensin(913) analogs |
TBA |
22197670 |
51 |
Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists. |
Kitasato University |
21967807 |
36 |
Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells. |
University of Pavia |
21889335 |
27 |
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet). |
Kitasato University |
21641219 |
12 |
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons. |
Kitasato University |
21481987 |
27 |
Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster |
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 |
21256034 |
58 |
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies. |
Kitasato University |
20850307 |
27 |
Design and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration. |
Kitasato University |
20685120 |
20 |
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. |
Kitasato University |
20483601 |
22 |
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology. |
Kitasato University |
19818611 |
100 |
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach. |
Schering-Plough Research Institute |
20056539 |
14 |
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology. |
Kitasato University |
20045339 |
16 |
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2). |
University of Pavia |
19827750 |
39 |
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1). |
Clinical Research Institute of Montreal |
19576786 |
129 |
Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands. |
Institute For Molecular Studies |
19620007 |
4 |
Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative. |
Kitasato University |
| 21 |
Arylacetamide kappa-selective opioid ligands |
TBA |
| 26 |
6N-Cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions |
TBA |
| 24 |
Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists |
TBA |
| 9 |
Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs |
TBA |
| 22 |
Palladium-catalyzed synthesis of C3-substituted 3-deoxymorphines. |
TBA |
| 6 |
New potent enkephalin analogs containing trifluoromethylamino acid residues |
TBA |
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 |
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 |
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 |
17166723 |
141 |
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties. |
Organon Laboratories |
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 |
15456245 |
44 |
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders. |
Johnson & Johnson Pharmaceutical Research & Development |
15324897 |
3 |
A novel cyclic enkephalin analogue with potent opioid antagonist activity. |
Clinical Research Institute of Montreal |
14695830 |
111 |
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors. |
Harvard Medical School |
12749896 |
47 |
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues. |
Rensselaer Polytechnic Institute |
12672226 |
9 |
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus. |
University of Maryland |
12593663 |
146 |
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines. |
Rensselaer Polytechnic Institute |
12383009 |
2 |
Kappa-opioid receptor model in a phospholipid bilayer: molecular dynamics simulation. |
University of Catania |
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 |
11755345 |
45 |
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives. |
Niddk |
11266156 |
42 |
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines. |
Rensselaer Polytechnic Institute |
32435370 |
45 |
Novel |
University of Catania |
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 |
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 |
31857840 |
92 |
Discovery of Axelopran (TD-1211): A Peripherally Restricted ?-Opioid Receptor Antagonist. |
Theravance Biopharma Us |
31550662 |
109 |
Progress in the development of more effective and safer analgesics for pain management. |
University of Catania |
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 |
30939014 |
143 |
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety. |
Universit£T M£Nster |
30924650 |
73 |
Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic ?-Opioid Receptor (MOR) Agonist/?-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability. |
University of Michigan |
30543421 |
74 |
Development of Novel Quinoxaline-Based ?-Opioid Receptor Agonists for the Treatment of Neuroinflammation. |
Universit£T M£Nster |
9873693 |
24 |
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists. |
Research Triangle Institute |
9873439 |
18 |
C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study. |
National Taiwan University |
31220675 |
88 |
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. |
Biological Research Centre of The Hungarian Academy of Sciences |
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 |
9276018 |
47 |
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution. |
Oregon State University |
9111295 |
48 |
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence. |
Oregon State University |
8893842 |
6 |
Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1(3-aminophenyl)-2-(1-pyrrolidi nyl) ethyl]acetamide: kappa opioid receptor agonists with limited access to the central nervous system. |
University of Minnesota |
8691442 |
52 |
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency. |
University of Arizona |
8676350 |
39 |
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2. |
University of Arizona |
8642554 |
42 |
Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids. |
Institute |
8632410 |
33 |
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors. |
Universitá |
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 |
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 |
8201586 |
3 |
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice. |
University of Minnesota |
24262888 |
105 |
The most effective influence of 17-(3-ethoxypropyl) substituent on the binding affinity and the agonistic activity in KNT-127 derivatives, ? opioid receptor agonists. |
Kitasato University |
8097539 |
10 |
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid. |
Oregon State University |
8096246 |
70 |
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
University of Arizona |
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 |
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 |
7966152 |
57 |
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11. |
University of Arizona |
23822516 |
142 |
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations. |
Universit£ |
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 |
7932535 |
40 |
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
National Taiwan University |
23517479 |
13 |
Orally active opioid compounds from a non-poppy source. |
Temple University |
23623711 |
82 |
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton having a 7-amide side chain and their pharmacologies. |
Kitasato University |
7861405 |
9 |
Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2. |
University of Arizona |
7799399 |
8 |
kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists. |
University of Minnesota |
7731019 |
16 |
Electrophilic N-benzylnaltrindoles as delta opioid receptor-selective antagonists. |
University of Minnesota |
7707326 |
39 |
Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids. |
Eastern Michigan University |
7658433 |
27 |
Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1. |
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 |
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 |
18249547 |
69 |
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties. |
Organon Laboratories |
11960505 |
18 |
Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
Chiba University |
29107424 |
27 |
Selective kappa opioid antagonists for treatment of addiction, are we there yet? |
University of Science and Technology |
29477074 |
79 |
Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review. |
University of Catania |
3020244 |
45 |
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors. |
TBA |
2876099 |
51 |
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties. |
TBA |
30350997 |
111 |
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic ? Receptor Ligands with Exocyclic Amino Moiety. |
Universit£T M£Nster |
28734666 |
23 |
Development of novel LP1-based analogues with enhanced delta opioid receptor profile. |
University of Catania |
1972964 |
40 |
Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
University of Arizona |
1895300 |
15 |
Modification of the enkephalin"message" with an artificial polycationic C-terminus. |
Case Western Reserve University |
1847432 |
13 |
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics. |
Anaquest |
1846921 |
56 |
(2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics. |
Zambeletti Research Laboratories |
1846918 |
12 |
2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists. |
Ici Pharmaceuticals Group |
1652025 |
45 |
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. |
Zambeletti Research Laboratories |
28522254 |
42 |
Novel delta opioid receptor agonists with oxazatricyclodecane structure showing potent agonistic activities. |
Kitasato University |
1652019 |
12 |
Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers. |
University of Washington |
28499731 |
100 |
Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of?-opioid receptor antagonists. |
Theravance Biopharma Us |
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 |
1315868 |
44 |
Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity. |
Harvard Medical School |
26496515 |
11 |
Iminothiazoline-Sulfonamide Hybrids as Jack Bean Urease Inhibitors; Synthesis, Kinetic Mechanism and Computational Molecular Modeling. |
Quaid-I-Azam University |
26520885 |
21 |
Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents. |
Hazara 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 |