A compound that exhibits agonist activity at the kappa-opioid receptor.
ChEBI ID: 59282
| Member | Definition | Class |
|---|---|---|
| butorphanol | Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain. | butorphanol |
| eluxadoline | An amino acid amide obtained by the formal condensation of the carboxy group of 4-carbamoyl-2,6-dimethyl-L-phenylalanine with the secondary amino group of 2-methoxy-5-({[(1S)-1-(4-phenylimidazol-2-yl)ethyl]amino}methyl)benzoic acid. It has mixed opioid receptor activity and is used for treatment of irritable bowel syndrome with diarrhoea. | eluxadoline |
| meperidine | A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain. | pethidine |
| meperidine hydrochloride | The hydrochloride salt of pethidine. An analgesic used for the treatment of postoperative and labour pain. | pethidine hydrochloride |
| noribogaine | An organic heteropentacyclic compound that is ibogamine in which the indole hydrogen para to the indole nitrogen has been replaced by a hydroxy group. It is the primary (and long-lived) metabolite of ibogaine, the psychoactive indole alkaloid found in the African rainforest shrub Tabernanthe iboga. | noribogaine |
| tramadol | A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. | (R,R)-tramadol |
| tramadol hydrochloride | A hydrochloride resulting from the reaction of (R,R)-tramadol with 1 molar equivalent of hydrogen chloride; the (R,R)-enantiomer of the racemic opioid analgesic tramadol hydrochloride, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. | (R,R)-tramadol hydrochloride |
| u 69593 | A monocarboxylic acid amide obtained by formal condensation between the carboxy group of phenylacetic acid and the secodary amino group of (5R,7S,8S)-N-methyl-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-amine. | U69593 |
| u-50488 | A monocarboxylic acid amide obtained by formal condensation between the carboxy group of 3,4-dichlorophenylacetic acid and the secondary amino group of (1R,2R)-N-methyl-2-(pyrrolidin-1-yl)cyclohexanamine | U50488 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 3,893 (33.33) | 18.7374 |
| 1990's | 2,297 (19.67) | 18.2507 |
| 2000's | 2,339 (20.03) | 29.6817 |
| 2010's | 2,329 (19.94) | 24.3611 |
| 2020's | 822 (7.04) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,794 (21.43%) | 5.53% |
| Reviews | 607 (4.66%) | 6.00% |
| Case Studies | 722 (5.54%) | 4.05% |
| Observational | 57 (0.44%) | 0.25% |
| Other | 8,857 (67.94%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 67.9K protein | Vaccinia virus | Potency | 8.9125 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 4.7755 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 16.1862 | 2 | 4 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 1.7377 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 7.7619 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 2.6200 | 1 | 2 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 5.0119 | 2 | 4 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 38.9018 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 18.2014 | 2 | 2 |
| G | Vesicular stomatitis virus | Potency | 1.7377 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 2 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 6.3096 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 10.6822 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 1.7377 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 1.7377 | 1 | 2 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 5.6114 | 2 | 2 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 12.5893 | 1 | 2 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 12.5893 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 1.7377 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 2 | 4 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 13.3714 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 16.0011 | 1 | 2 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 89.1251 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 10.8573 | 2 | 3 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 1 | 1 |
| Acyl-CoA desaturase 1 | Rattus norvegicus (Norway rat) | Ki | 0.0035 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 0.7175 | 1 | 4 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 134.0000 | 2 | 2 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.0550 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 | 8.0402 | 7 | 9 |
| Delta-type opioid receptor | Mus musculus (house mouse) | IC50 | 20.2500 | 2 | 2 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 8.7167 | 2 | 3 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 6.0258 | 18 | 26 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 2.5000 | 5 | 6 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 2.5006 | 2 | 2 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.0396 | 3 | 5 |
| Kappa-type opioid receptor | Homo sapiens (human) | IC50 | 1.9960 | 20 | 22 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | IC50 | 8.1016 | 4 | 5 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 4.3587 | 5 | 6 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0181 | 15 | 21 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.2854 | 40 | 68 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0081 | 1 | 1 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 7 | 7 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.5660 | 3 | 4 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 | 5.2006 | 7 | 8 |
| Mu-type opioid receptor | Mus musculus (house mouse) | IC50 | 20.2500 | 2 | 2 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 8.7167 | 2 | 3 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.3960 | 9 | 24 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 1.7707 | 14 | 15 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ki | 0.3672 | 6 | 11 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 1.3345 | 5 | 6 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Nociceptin receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.6920 | 1 | 1 |
| Nociceptin receptor | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 50.1041 | 3 | 3 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | Ki | 17.8000 | 2 | 2 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | Ki | 0.4127 | 3 | 3 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 55.5050 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Amine oxidase [flavin-containing] A | Rattus norvegicus (Norway rat) | EC50 | 0.3300 | 1 | 1 |
| Amine oxidase [flavin-containing] B | Rattus norvegicus (Norway rat) | EC50 | 0.3300 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | EC50 | 10.0000 | 2 | 2 |
| Delta-type opioid receptor | Homo sapiens (human) | Kd | 1.9800 | 2 | 2 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | EC50 | 1.4454 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 | 0.1340 | 62 | 89 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | EC50 | 1.6365 | 3 | 3 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 | 0.0077 | 1 | 1 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kd | 4.8940 | 2 | 2 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.0010 | 1 | 1 |
| Mitogen-activated protein kinase 10 | Homo sapiens (human) | EC50 | 1.2400 | 1 | 1 |
| Mitogen-activated protein kinase 8 | Homo sapiens (human) | EC50 | 1.2400 | 1 | 1 |
| Mitogen-activated protein kinase 9 | Homo sapiens (human) | EC50 | 1.2400 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | EC50 | 0.0332 | 2 | 3 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 | 5.0482 | 5 | 5 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kd | 1.2672 | 4 | 5 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Activity | 25.0000 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | ED50 | 1.9800 | 1 | 2 |
| Delta-type opioid receptor | Homo sapiens (human) | Emax | 0.1780 | 2 | 5 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0412 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | ED50 | 0.0255 | 2 | 2 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Emax | 0.0580 | 1 | 1 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0078 | 2 | 2 |
| Liver carboxylesterase 1 | Homo sapiens (human) | Km | 1,900.0000 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | ED50 | 1.7775 | 2 | 4 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Emax | 0.1703 | 4 | 6 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0315 | 1 | 1 |