Page last updated: 2024-08-07 16:37:19
Kappa-type opioid receptor
A kappa-type opioid receptor that is encoded in the genome of guinea pig. [OMA:P41144, PRO:DNx]
Synonyms
K-OR-1;
KOR-1
Research
Bioassay Publications (134)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 9 (6.72) | 18.7374 |
| 1990's | 52 (38.81) | 18.2507 |
| 2000's | 37 (27.61) | 29.6817 |
| 2010's | 33 (24.63) | 24.3611 |
| 2020's | 3 (2.24) | 2.80 |
Compounds (132)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bremazocine | Cavia porcellus (domestic guinea pig) | IC50 | 0.0012 | 1 | 1 |
| cgp 52411 | Cavia porcellus (domestic guinea pig) | IC50 | 4.5000 | 1 | 1 |
| acetazolamide | Cavia porcellus (domestic guinea pig) | Ki | 0.2500 | 1 | 1 |
| aurintricarboxylic acid | Cavia porcellus (domestic guinea pig) | IC50 | 282.9000 | 1 | 1 |
| verapamil | Cavia porcellus (domestic guinea pig) | Ki | 1.7500 | 1 | 1 |
| fentanyl | Cavia porcellus (domestic guinea pig) | IC50 | 5.8930 | 1 | 1 |
| fentanyl | Cavia porcellus (domestic guinea pig) | Ki | 0.1965 | 1 | 1 |
| gr 89696 | Cavia porcellus (domestic guinea pig) | Ki | 0.0005 | 1 | 1 |
| haloperidol | Cavia porcellus (domestic guinea pig) | Ki | 0.0026 | 1 | 1 |
| nevirapine | Cavia porcellus (domestic guinea pig) | IC50 | 0.7000 | 1 | 1 |
| 1,3-ditolylguanidine | Cavia porcellus (domestic guinea pig) | Ki | 0.0710 | 1 | 1 |
| galantamine | Cavia porcellus (domestic guinea pig) | IC50 | 3.2000 | 1 | 1 |
| oleanolic acid | Cavia porcellus (domestic guinea pig) | IC50 | 120.0000 | 1 | 1 |
| Berberine chloride (TN) | Cavia porcellus (domestic guinea pig) | IC50 | 0.3740 | 1 | 1 |
| alfentanil | Cavia porcellus (domestic guinea pig) | IC50 | 10.0000 | 1 | 3 |
| haloperidol decanoate | Cavia porcellus (domestic guinea pig) | Ki | 0.0035 | 1 | 1 |
| spiradoline | Cavia porcellus (domestic guinea pig) | Ki | 0.0142 | 2 | 3 |
| efavirenz | Cavia porcellus (domestic guinea pig) | IC50 | 0.0180 | 1 | 1 |
| alpha-amyrin | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| enkephalin, d-penicillamine (2,5)- | Cavia porcellus (domestic guinea pig) | Ki | 0.3053 | 1 | 2 |
| u 69593 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0021 | 1 | 3 |
| u 69593 | Cavia porcellus (domestic guinea pig) | Ki | 0.0046 | 3 | 4 |
| tifluadom | Cavia porcellus (domestic guinea pig) | Ki | 0.0008 | 1 | 2 |
| bw 373u86 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0003 | 1 | 1 |
| marimastat | Cavia porcellus (domestic guinea pig) | IC50 | 0.0031 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | IC50 | 3.2800 | 4 | 5 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | Ki | 7.6175 | 2 | 4 |
| 2-(3,4-dichlorophenyl)-n-methyl-n-(1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl)acetamide | Cavia porcellus (domestic guinea pig) | IC50 | 0.0022 | 1 | 1 |
| ly 99335, (3r-cis)-isomer | Cavia porcellus (domestic guinea pig) | Ki | 0.8330 | 3 | 3 |
| ly 106737 | Cavia porcellus (domestic guinea pig) | Ki | 0.0520 | 2 | 2 |
| enkephalin, pen(2,5)-4-chloro-phe(4)- | Cavia porcellus (domestic guinea pig) | IC50 | 0.0016 | 1 | 1 |
| etravirine | Cavia porcellus (domestic guinea pig) | IC50 | 0.0970 | 1 | 1 |
| dapivirine | Cavia porcellus (domestic guinea pig) | IC50 | 0.3220 | 1 | 1 |
| ginsenoside re | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| enkephalin, leucine | Cavia porcellus (domestic guinea pig) | Ki | 10.0000 | 1 | 2 |
| buprenorphine | Cavia porcellus (domestic guinea pig) | Ki | 0.0000 | 1 | 1 |
| etorphine | Cavia porcellus (domestic guinea pig) | IC50 | 0.0018 | 1 | 1 |
| 2-(3,4-dihydroxyphenyl)-7,8-dihydroxy-1-benzopyran-4-one | Cavia porcellus (domestic guinea pig) | IC50 | 0.7400 | 1 | 1 |
| mitragynine | Cavia porcellus (domestic guinea pig) | Ki | 1.0000 | 1 | 1 |
| u-50488 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0958 | 2 | 2 |
| u-50488 | Cavia porcellus (domestic guinea pig) | Ki | 0.0191 | 13 | 16 |
| tandutinib | Cavia porcellus (domestic guinea pig) | IC50 | 0.2000 | 1 | 1 |
| ketazocine | Cavia porcellus (domestic guinea pig) | Ki | 0.0010 | 1 | 1 |
| ici 199441 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0036 | 3 | 4 |
| dynorphin (1-11) | Cavia porcellus (domestic guinea pig) | IC50 | 0.2840 | 1 | 1 |
| brl 52537 | Cavia porcellus (domestic guinea pig) | Ki | 0.0002 | 1 | 1 |
| quercetin | Cavia porcellus (domestic guinea pig) | IC50 | 1.0000 | 1 | 1 |
| luteolin | Cavia porcellus (domestic guinea pig) | IC50 | 0.6600 | 1 | 1 |
| harmine | Cavia porcellus (domestic guinea pig) | IC50 | 5.0360 | 2 | 2 |
| nalmefene | Cavia porcellus (domestic guinea pig) | Ki | 0.0020 | 1 | 1 |
| nalorphine | Cavia porcellus (domestic guinea pig) | Ki | 0.0150 | 1 | 1 |
| naloxone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0500 | 1 | 1 |
| naloxone | Cavia porcellus (domestic guinea pig) | Ki | 0.0435 | 5 | 5 |
| oxycodone | Cavia porcellus (domestic guinea pig) | IC50 | 76.2000 | 1 | 1 |
| oxymorphone | Cavia porcellus (domestic guinea pig) | Ki | 0.5039 | 2 | 3 |
| morphine | Cavia porcellus (domestic guinea pig) | IC50 | 0.9308 | 5 | 6 |
| morphine | Cavia porcellus (domestic guinea pig) | Ki | 4.6570 | 20 | 26 |
| 7-benzylidenenaltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0213 | 3 | 3 |
| endomorphin 1 | Cavia porcellus (domestic guinea pig) | Ki | 3.7115 | 2 | 2 |
| endomorphin 2 | Cavia porcellus (domestic guinea pig) | IC50 | 1.0000 | 1 | 1 |
| endomorphin 2 | Cavia porcellus (domestic guinea pig) | Ki | 2.7080 | 1 | 1 |
| lysophosphatidic acid | Cavia porcellus (domestic guinea pig) | IC50 | 0.4998 | 1 | 1 |
| levorphanol | Cavia porcellus (domestic guinea pig) | Ki | 5.0026 | 3 | 5 |
| levallorphan | Cavia porcellus (domestic guinea pig) | Ki | 12.0000 | 1 | 1 |
| cyclorphan | Cavia porcellus (domestic guinea pig) | Ki | 0.0010 | 2 | 4 |
| naltrexone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0093 | 6 | 8 |
| naltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0042 | 21 | 28 |
| dextrorphan | Cavia porcellus (domestic guinea pig) | Ki | 20.0000 | 1 | 1 |
| methylnaltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0200 | 1 | 1 |
| n-methylnaltrindole | Cavia porcellus (domestic guinea pig) | Ki | 0.0083 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | Ki | 5.0000 | 1 | 1 |
| norbinaltorphimine | Cavia porcellus (domestic guinea pig) | Ki | 0.0288 | 11 | 17 |
| dermorphin | Cavia porcellus (domestic guinea pig) | IC50 | 10.0000 | 1 | 1 |
| 6 beta-hydroxynaltrexone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0081 | 2 | 3 |
| 14-methoxymetopon | Cavia porcellus (domestic guinea pig) | Ki | 0.0378 | 2 | 5 |
| alvimopan anhydrous | Cavia porcellus (domestic guinea pig) | Ki | 0.0050 | 1 | 1 |
| oxymorphindole | Cavia porcellus (domestic guinea pig) | Ki | 0.3950 | 1 | 1 |
| naltrindole | Cavia porcellus (domestic guinea pig) | Ki | 0.0199 | 18 | 18 |
| cyprodime | Cavia porcellus (domestic guinea pig) | Ki | 0.1096 | 1 | 1 |
| 6alpha-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5alpha-epoxymorphinan | Cavia porcellus (domestic guinea pig) | IC50 | 0.0100 | 2 | 3 |
| 6alpha-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5alpha-epoxymorphinan | Cavia porcellus (domestic guinea pig) | Ki | 0.0038 | 2 | 3 |
| 7-benzylidenenaltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0339 | 3 | 3 |
| clocinnamox | Cavia porcellus (domestic guinea pig) | Ki | 0.0027 | 1 | 1 |
| cgp 53353 | Cavia porcellus (domestic guinea pig) | IC50 | 2.2000 | 1 | 1 |
| enkephalin, leucine-2-alanine | Cavia porcellus (domestic guinea pig) | IC50 | 1.4691 | 2 | 3 |
| binodenoson | Cavia porcellus (domestic guinea pig) | Ki | 430.0000 | 1 | 1 |
| sodium selenate | Cavia porcellus (domestic guinea pig) | Ki | 0.0030 | 2 | 4 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Cavia porcellus (domestic guinea pig) | Ki | 0.0002 | 1 | 1 |
| ginsenoside rb1 | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| ly 255582 | Cavia porcellus (domestic guinea pig) | Ki | 0.0173 | 4 | 5 |
| ginsenoside f2 | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| ginsenoside rg3 | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| bibr 1532 | Cavia porcellus (domestic guinea pig) | IC50 | 11.5700 | 1 | 1 |
| tan 67 | Cavia porcellus (domestic guinea pig) | Ki | 0.2841 | 1 | 1 |
| leucettamine b | Cavia porcellus (domestic guinea pig) | IC50 | 5.0330 | 2 | 2 |
| deltorphin i, ala(2)- | Cavia porcellus (domestic guinea pig) | Ki | 10.0000 | 1 | 1 |
| 8-carboxamidocyclazocine | Cavia porcellus (domestic guinea pig) | Ki | 0.0005 | 2 | 2 |
| 6-deoxy-6-fluoronaltrexone | Cavia porcellus (domestic guinea pig) | IC50 | 0.0369 | 2 | 2 |
| 6-deoxy-6-fluoronaltrexone | Cavia porcellus (domestic guinea pig) | Ki | 0.0103 | 2 | 3 |
| dynorphin a (1-11)-amide | Cavia porcellus (domestic guinea pig) | IC50 | 0.0006 | 1 | 1 |
| dynorphin a (1-11)-amide | Cavia porcellus (domestic guinea pig) | Ki | 0.0001 | 1 | 2 |
| eluxadoline | Cavia porcellus (domestic guinea pig) | Ki | 0.0550 | 1 | 1 |
| ki 8751 | Cavia porcellus (domestic guinea pig) | IC50 | 2.4000 | 1 | 1 |
| ginsenoside rd | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| ginsenoside rb3 | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| 14-o-methyloxymorphone | Cavia porcellus (domestic guinea pig) | Ki | 0.0102 | 1 | 1 |
| methylnaloxonium iodide | Cavia porcellus (domestic guinea pig) | Ki | 1.0000 | 1 | 1 |
| sgi 1776 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0690 | 1 | 1 |
| dynorphins | Cavia porcellus (domestic guinea pig) | Ki | 0.0011 | 2 | 4 |
| gsk 1363089 | Cavia porcellus (domestic guinea pig) | IC50 | 2.9900 | 1 | 1 |
| 7-hydroxymitragynine | Cavia porcellus (domestic guinea pig) | Ki | 0.1590 | 2 | 2 |
| 7-spiroindanyloxymorphone | Cavia porcellus (domestic guinea pig) | Ki | 0.5880 | 2 | 2 |
| gypenoside XVII | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| (20R)-ginsenoside Rg3 | Cavia porcellus (domestic guinea pig) | IC50 | 250.0000 | 1 | 1 |
| urb937 | Cavia porcellus (domestic guinea pig) | IC50 | 0.0020 | 1 | 1 |
| 3-(2-((cyclobutylmethyl)(phenethyl)amino)ethyl)phenol | Cavia porcellus (domestic guinea pig) | Ki | 0.0019 | 1 | 1 |
| ((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one) | Cavia porcellus (domestic guinea pig) | IC50 | 5.0355 | 2 | 2 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| penicillin g | Cavia porcellus (domestic guinea pig) | Km | 51.0000 | 1 | 1 |
| cephalothin | Cavia porcellus (domestic guinea pig) | Km | 62.0000 | 1 | 1 |
| amoxicillin | Cavia porcellus (domestic guinea pig) | Km | 84.0000 | 1 | 1 |
| ticarcillin | Cavia porcellus (domestic guinea pig) | Km | 10.0000 | 1 | 1 |
| piperacillin | Cavia porcellus (domestic guinea pig) | Km | 90.0000 | 1 | 1 |
| imipenem, anhydrous | Cavia porcellus (domestic guinea pig) | Km | 2,977.0000 | 1 | 1 |
| sr141716 | Cavia porcellus (domestic guinea pig) | Kb | 0.0007 | 1 | 2 |
| u 69593 | Cavia porcellus (domestic guinea pig) | Emax | 0.0580 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | ED50 | 0.6290 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Cavia porcellus (domestic guinea pig) | Emax | 0.1430 | 2 | 3 |
| 7-benzylidenenaltrexone | Cavia porcellus (domestic guinea pig) | Ke | 0.0353 | 2 | 3 |
| naltrexone | Cavia porcellus (domestic guinea pig) | Ke | 0.0041 | 3 | 5 |
| n-methylnaltrindole | Cavia porcellus (domestic guinea pig) | Ke | 0.0200 | 1 | 2 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | ED50 | 0.5090 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Cavia porcellus (domestic guinea pig) | Emax | 0.1350 | 2 | 3 |
| cefuroxime | Cavia porcellus (domestic guinea pig) | Km | 88.0000 | 1 | 1 |
| cefepime | Cavia porcellus (domestic guinea pig) | Km | 2,685.0000 | 1 | 1 |
| hr 810 | Cavia porcellus (domestic guinea pig) | Km | 304.0000 | 1 | 1 |
| norbinaltorphimine | Cavia porcellus (domestic guinea pig) | Ke | 0.0002 | 7 | 10 |
| ceftazidime | Cavia porcellus (domestic guinea pig) | Km | 1,749.0000 | 1 | 1 |
| binaltorphimine | Cavia porcellus (domestic guinea pig) | Ke | 0.0056 | 2 | 2 |
| naltrexone hydrochloride | Cavia porcellus (domestic guinea pig) | Ke | 0.0212 | 2 | 2 |
| oxymorphindole | Cavia porcellus (domestic guinea pig) | Ke | 0.1670 | 1 | 2 |
| naltrindole | Cavia porcellus (domestic guinea pig) | Ke | 0.0167 | 6 | 11 |
| cefotaxime | Cavia porcellus (domestic guinea pig) | Km | 714.0000 | 1 | 1 |
| aztreonam | Cavia porcellus (domestic guinea pig) | Km | 938.0000 | 1 | 1 |
| cyprodime | Cavia porcellus (domestic guinea pig) | Ke | 1.1570 | 1 | 1 |
| 7-benzylidenenaltrexone | Cavia porcellus (domestic guinea pig) | Ke | 0.0337 | 2 | 3 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Cavia porcellus (domestic guinea pig) | Ke | 0.0002 | 1 | 1 |
| ly 255582 | Cavia porcellus (domestic guinea pig) | Ke | 0.0003 | 1 | 2 |
| ici 174865 | Cavia porcellus (domestic guinea pig) | Ke | 0.8360 | 2 | 3 |
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Discovery of κ Opioid Receptor (KOR)-Selective d-Tetrapeptides with Improved ACS medicinal chemistry letters, , Nov-10, Volume: 13, Issue:11, 2022
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.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
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.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
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.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
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.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
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.Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
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.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
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.Journal of medicinal chemistry, , Aug-29, Volume: 40, Issue:18, 1997
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.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
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.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Synthesis of 8-aminomorphans with high KOR affinity.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Evaluation of N-substitution in 6,7-benzomorphan compounds.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
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.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists.Journal of medicinal chemistry, , Jun-25, Volume: 36, Issue:13, 1993
Selective reversible and irreversible ligands for the kappa opioid receptor.Journal of medicinal chemistry, , Jun-12, Volume: 35, Issue:12, 1992
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.Journal of medicinal chemistry, , Aug-07, Volume: 35, Issue:16, 1992
(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.Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
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.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
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.Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
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.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
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.Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
Synthesis of 8-aminomorphans with high KOR affinity.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.Journal of medicinal chemistry, , Sep-16, Volume: 37, Issue:19, 1994
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
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Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.Journal of medicinal chemistry, , Aug-24, Volume: 49, Issue:17, 2006
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3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.Bioorganic & medicinal chemistry letters, , Jul-09, Volume: 11, Issue:13, 2001
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N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
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(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
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3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
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Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
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.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.Journal of medicinal chemistry, , Dec-09, Volume: 37, Issue:25, 1994
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
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.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
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.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
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.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.Bioorganic & medicinal chemistry letters, , Apr-09, Volume: 11, Issue:7, 2001
Delta opioid binding selectivity of 3-ether analogs of naltrindole.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 9, Issue:24, 1999
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
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Synthesis of 7-arylmorphinans. Probing the "address" requirements for selectivity at opioid delta receptors.Journal of medicinal chemistry, , Jul-30, Volume: 41, Issue:16, 1998
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.Journal of medicinal chemistry, , Mar-04, Volume: 37, Issue:5, 1994
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.Journal of medicinal chemistry, , Volume: 33, Issue:6, 1990
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
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(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.Journal of medicinal chemistry, , Mar-04, Volume: 37, Issue:5, 1994
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.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
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.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.Journal of medicinal chemistry, , Volume: 29, Issue:4, 1986
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.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
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.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
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A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993