Page last updated: 2024-08-07 16:32:08
Kappa-type opioid receptor
A kappa-type opioid receptor that is encoded in the genome of rat. [OMA:P34975, PRO:DNx]
Synonyms
K-OR-1;
KOR-1
Research
Bioassay Publications (54)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 15 (27.78) | 18.7374 |
| 1990's | 8 (14.81) | 18.2507 |
| 2000's | 18 (33.33) | 29.6817 |
| 2010's | 10 (18.52) | 24.3611 |
| 2020's | 3 (5.56) | 2.80 |
Compounds (52)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fentanyl | Rattus norvegicus (Norway rat) | IC50 | 0.0122 | 4 | 5 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 7.0700 | 2 | 3 |
| ondansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| 1,3-ditolylguanidine | Rattus norvegicus (Norway rat) | Ki | 3.9500 | 1 | 1 |
| fluorodeoxyuridylate | Rattus norvegicus (Norway rat) | Ki | 0.0140 | 1 | 1 |
| ketobemidone | Rattus norvegicus (Norway rat) | IC50 | 7.0000 | 1 | 1 |
| etonitazene | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 1 | 2 |
| sufentanil | Rattus norvegicus (Norway rat) | IC50 | 0.0023 | 1 | 1 |
| carfentanil | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 1 | 2 |
| bromodeoxyuridylate | Rattus norvegicus (Norway rat) | Ki | 1.4000 | 1 | 1 |
| u 69593 | Rattus norvegicus (Norway rat) | IC50 | 0.0006 | 1 | 1 |
| u 69593 | Rattus norvegicus (Norway rat) | Ki | 0.0026 | 5 | 5 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Rattus norvegicus (Norway rat) | IC50 | 3.6010 | 1 | 1 |
| 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide | Rattus norvegicus (Norway rat) | Ki | 3.5350 | 1 | 1 |
| methotrexate | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 1 | 1 |
| salvinorin a | Rattus norvegicus (Norway rat) | Ki | 0.4921 | 22 | 23 |
| 5-nitro-2'-deoxyuridine 5'-monophosphate | Rattus norvegicus (Norway rat) | Ki | 0.0290 | 1 | 1 |
| 5-trifluoromethyl-2'-deoxyuridylic acid | Rattus norvegicus (Norway rat) | Ki | 0.0390 | 1 | 1 |
| deltorphin ii, ile(5,6)- | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| enkephalin, methionine | Rattus norvegicus (Norway rat) | IC50 | 0.1290 | 2 | 2 |
| 5-iodo-2'-deoxyuridine 5'-monophosphate | Rattus norvegicus (Norway rat) | Ki | 1.6000 | 1 | 1 |
| enkephalin, leucine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 2 |
| etorphine | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 1 | 1 |
| u-50488 | Rattus norvegicus (Norway rat) | IC50 | 5.2303 | 4 | 5 |
| u-50488 | Rattus norvegicus (Norway rat) | Ki | 0.0005 | 2 | 2 |
| dynorphin (1-11) | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 1 | 1 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Rattus norvegicus (Norway rat) | Ki | 0.0500 | 1 | 1 |
| nalorphine | Rattus norvegicus (Norway rat) | IC50 | 0.0040 | 2 | 2 |
| naloxone | Rattus norvegicus (Norway rat) | IC50 | 0.0018 | 3 | 4 |
| oxycodone | Rattus norvegicus (Norway rat) | Ki | 2.6580 | 1 | 1 |
| oxymorphone | Rattus norvegicus (Norway rat) | Ki | 0.2460 | 3 | 3 |
| morphine | Rattus norvegicus (Norway rat) | IC50 | 0.0545 | 8 | 9 |
| morphine | Rattus norvegicus (Norway rat) | Ki | 0.1130 | 2 | 2 |
| endomorphin 1 | Rattus norvegicus (Norway rat) | Ki | 6.6842 | 3 | 3 |
| endomorphin 2 | Rattus norvegicus (Norway rat) | Ki | 6.6702 | 3 | 3 |
| levallorphan | Rattus norvegicus (Norway rat) | IC50 | 0.0008 | 1 | 2 |
| naltrexone | Rattus norvegicus (Norway rat) | IC50 | 0.0005 | 2 | 3 |
| naltrexone | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 4 | 5 |
| norbinaltorphimine | Rattus norvegicus (Norway rat) | Ki | 0.0019 | 7 | 8 |
| naltrindole | Rattus norvegicus (Norway rat) | Ki | 0.0186 | 4 | 4 |
| cyprodime | Rattus norvegicus (Norway rat) | IC50 | 0.0472 | 1 | 2 |
| 3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(-)-isomer | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 1 | 1 |
| cilansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Rattus norvegicus (Norway rat) | Ki | 0.0022 | 10 | 10 |
| 6'-guanidinonaltrindole | Rattus norvegicus (Norway rat) | Ki | 0.0049 | 3 | 3 |
| dynorphin a (1-11)-amide | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 3 | 3 |
| 5-chloro-2'-deoxyuridine 5'-triphosphate | Rattus norvegicus (Norway rat) | Ki | 0.1900 | 1 | 1 |
| dynorphins | Rattus norvegicus (Norway rat) | Ki | 0.0015 | 4 | 4 |
| 7-spiroindanyloxymorphone | Rattus norvegicus (Norway rat) | Ki | 0.2783 | 3 | 3 |
| cj 15,208 | Rattus norvegicus (Norway rat) | Ki | 0.0327 | 3 | 3 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| metergoline | Rattus norvegicus (Norway rat) | Activity | 0.0632 | 1 | 1 |
| morphine | Rattus norvegicus (Norway rat) | Activity | 0.0030 | 1 | 1 |
Probes for narcotic receptor mediated phenomena. 12. cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for delta opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity.Journal of medicinal chemistry, , Volume: 29, Issue:6, 1986
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
Synthesis and stereochemistry of 7-phenyl-2-propionanilidobenzo[a]quinolizidine derivatives. Structural probes of fentanyl analgesics.Journal of medicinal chemistry, , Volume: 24, Issue:1, 1981
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.Bioorganic & medicinal chemistry, , Jul-15, Volume: 23, Issue:14, 2015
Novel cyclic biphalin analogue with improved antinociceptive properties.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
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.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.Bioorganic & medicinal chemistry, , Sep-01, Volume: 17, Issue:17, 2009
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
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 10, Issue:8, 2000
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
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
Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties.Journal of medicinal chemistry, , Volume: 26, Issue:1, 1983
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.Journal of medicinal chemistry, , Volume: 21, Issue:1, 1978
Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
3,7-Diazabicyclane: a new narcotic analgesic.Journal of medicinal chemistry, , Volume: 29, Issue:10, 1986
Novel nonnarcotic analgesics with an improved therapeutic ratio. Structure-activity relationships of 8-(methylthio)- and 8-(acylthio)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines.Journal of medicinal chemistry, , Volume: 28, Issue:11, 1985
Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties.Journal of medicinal chemistry, , Volume: 26, Issue:1, 1983
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
Synthesis and stereochemistry of 7-phenyl-2-propionanilidobenzo[a]quinolizidine derivatives. Structural probes of fentanyl analgesics.Journal of medicinal chemistry, , Volume: 24, Issue:1, 1981
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.Journal of medicinal chemistry, , Volume: 21, Issue:1, 1978
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.Journal of medicinal chemistry, , Volume: 21, Issue:5, 1978
N-(2,4,5-Trihydroxyphenehtyl)normetazocine, a potential irreversible inhibitor of the narcotic receptor.Journal of medicinal chemistry, , Volume: 20, Issue:5, 1977
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.Bioorganic & medicinal chemistry, , 05-01, Volume: 28, Issue:9, 2020
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.Bioorganic & medicinal chemistry, , 05-01, Volume: 28, Issue:9, 2020
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.Journal of medicinal chemistry, , Volume: 21, Issue:1, 1978
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.Bioorganic & medicinal chemistry letters, , Nov-06, Volume: 10, Issue:21, 2000
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.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.Journal of medicinal chemistry, , Mar-15, Volume: 44, Issue:6, 2001
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.Journal of medicinal chemistry, , Sep-24, Volume: 52, Issue:18, 2009
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.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Development of κ opioid receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013