Any compound that exhibits antagonist activity at the delta-opioid receptor.
ChEBI ID: 59283
| Member | Definition | Class |
|---|---|---|
| buprenorphine | A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain. | buprenorphine |
| 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 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 535 (8.13) | 18.7374 |
| 1990's | 608 (9.24) | 18.2507 |
| 2000's | 1,370 (20.83) | 29.6817 |
| 2010's | 2,308 (35.09) | 24.3611 |
| 2020's | 1,757 (26.71) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,234 (16.79%) | 5.53% |
| Reviews | 764 (10.40%) | 6.00% |
| Case Studies | 429 (5.84%) | 4.05% |
| Observational | 100 (1.36%) | 0.25% |
| Other | 4,821 (65.61%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.0550 | 1 | 1 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0013 | 1 | 1 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0275 | 2 | 2 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0009 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Delta-type opioid receptor | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 | 0.0010 | 1 | 1 |