Any compound that exhibits antagonist activity at the mu-opioid receptor
ChEBI ID: 50137
| Member | Definition | Class |
|---|---|---|
| nalbuphine | nalbuphine | |
| naloxegol | An organic heteropentacyclic compound that is naloxone in which the keto group is replaced by a PEG moiety. Used for treatment of opioid-induced constipation. | naloxegol |
| naloxone | A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | naloxone |
| naloxone hydrochloride | A hydrochloride resulting from the formal reaction of equimolar amounts of naloxone and hydrogen chloride. A specific opioid antagonist, it is used to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | naloxone hydrochloride |
| naltrexone | An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence. | naltrexone |
| naltrexone hydrochloride | A hydrochloride obtained by reaction of oxycodone with one molar equivalent of hydrochloric acid. it is a mu-opioid receptor antagonist that is used to treat alcohol dependence. | naltrexone hydrochloride |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 9,482 (35.87) | 18.7374 |
| 1990's | 5,890 (22.28) | 18.2507 |
| 2000's | 4,574 (17.30) | 29.6817 |
| 2010's | 4,651 (17.59) | 24.3611 |
| 2020's | 1,839 (6.96) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,775 (9.32%) | 5.53% |
| Reviews | 1,662 (5.58%) | 6.00% |
| Case Studies | 1,054 (3.54%) | 4.05% |
| Observational | 77 (0.26%) | 0.25% |
| Other | 24,215 (81.30%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 27.8381 | 3 | 3 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 1.2995 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 69.6219 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 15.8239 | 1 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 29.5635 | 5 | 5 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| GLS protein | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 10.6822 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 25.1547 | 2 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 24.1344 | 2 | 3 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 21.5491 | 2 | 3 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 25.1189 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 1.4125 | 1 | 1 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 47.3936 | 1 | 2 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 70.7946 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 10 kDa chaperonin | Escherichia coli | IC50 | 175.0000 | 2 | 2 |
| 10 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 3A | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| 5-hydroxytryptamine receptor 3B | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| 5-hydroxytryptamine receptor 3C | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| 5-hydroxytryptamine receptor 3D | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| 5-hydroxytryptamine receptor 3E | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli K-12 | IC50 | 250.0000 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli | IC50 | 175.0000 | 2 | 2 |
| 60 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 50.0000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.0055 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 454.2500 | 3 | 4 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 1.5000 | 1 | 2 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 20.0000 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 | 0.1538 | 23 | 35 |
| Delta-type opioid receptor | Mus musculus (house mouse) | IC50 | 50.0160 | 4 | 10 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0148 | 4 | 11 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.0826 | 56 | 72 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0456 | 9 | 10 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0402 | 9 | 12 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.0138 | 6 | 9 |
| Kappa-type opioid receptor | Homo sapiens (human) | IC50 | 0.0508 | 15 | 24 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | IC50 | 250.0030 | 2 | 2 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0013 | 3 | 7 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0101 | 23 | 33 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.0129 | 39 | 49 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0027 | 3 | 4 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 4 | 5 |
| kappa-type opioid receptor isoform 1 | Homo sapiens (human) | IC50 | 0.3680 | 2 | 4 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.0025 | 3 | 4 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 | 0.0235 | 26 | 40 |
| Mu-type opioid receptor | Mus musculus (house mouse) | IC50 | 100.0077 | 5 | 5 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0013 | 3 | 7 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0012 | 18 | 23 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0096 | 53 | 68 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0013 | 12 | 13 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0024 | 14 | 21 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 1 | 5 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 1 | 5 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 1 | 5 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 1 | 5 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 1 | 5 |
| Nociceptin receptor | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | Ki | 0.1030 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 1 | 1 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 157.5100 | 1 | 1 |
| Thiosulfate sulfurtransferase | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 2 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 2 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 31.5000 | 1 | 2 |
| Beta-galactosidase | Escherichia coli | EC50 | 31.5000 | 1 | 2 |
| Delta-type opioid receptor | Homo sapiens (human) | EC50 | 0.0091 | 4 | 4 |
| Delta-type opioid receptor | Mus musculus (house mouse) | EC50 | 0.0044 | 1 | 1 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 | 0.0010 | 1 | 2 |
| Delta-type opioid receptor | Homo sapiens (human) | Kd | 0.0013 | 2 | 2 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Kd | 0.0002 | 1 | 1 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.1200 | 2 | 4 |
| Histidine decarboxylase | Rattus norvegicus (Norway rat) | EC50 | 0.0010 | 1 | 2 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 | 0.0467 | 7 | 9 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | EC50 | 0.0008 | 1 | 1 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 | 0.0010 | 1 | 2 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0180 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.0935 | 3 | 5 |
| kappa-type opioid receptor isoform 1 | Homo sapiens (human) | EC50 | 5.0000 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | EC50 | 0.0019 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 | 0.0154 | 4 | 5 |
| Mu-type opioid receptor | Mus musculus (house mouse) | EC50 | 0.0002 | 2 | 2 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 | 0.0010 | 1 | 2 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0002 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | Kd | 0.0004 | 4 | 4 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.0784 | 4 | 6 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 2D6 | Homo sapiens (human) | Kb | 0.0006 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | Kb | 0.0111 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | Ke | 0.0283 | 9 | 9 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0382 | 10 | 14 |
| Kappa-type opioid receptor | Homo sapiens (human) | Kb | 0.0030 | 1 | 1 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ke | 0.0090 | 5 | 7 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ke | 0.0040 | 11 | 11 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0159 | 1 | 2 |
| Kappa-type opioid receptor | Homo sapiens (human) | pA2 | 0.0097 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | Kb | 0.0006 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ke | 0.0010 | 5 | 6 |
| Mu-type opioid receptor | Homo sapiens (human) | Ke | 0.0020 | 19 | 20 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0008 | 2 | 2 |
| UDP-glucuronosyltransferase 1A1 | Homo sapiens (human) | Km | 1,310.0000 | 1 | 1 |
| UDP-glucuronosyltransferase 1A8 | Homo sapiens (human) | Km | 1,000.0000 | 1 | 2 |