| Systematic (IUPAC) name | |
|---|---|
| N-[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]-L-alanine | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Non-regulated |
| Identifiers | |
| CAS number | 92175-57-0 |
| ATC code | None |
| PubChem | CID 123982 |
| DrugBank | DB08040 |
| ChemSpider | 110501 |
| Chemical data | |
| Formula | C14H18N2O5 |
| Mol. mass | 294.303 g/mol |
| SMILES | eMolecules & PubChem |
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Kelatorphan is a drug which acts as a powerful and complete inhibitor of nearly all of the enzymes responsible for catabolism of the endogenous enkephalins, including neutral endopeptidase (NEP), dipeptidyl peptidase III (DPP3), aminopeptidase N (APN), and angiotensin-converting enzyme (ACE).[1][2][3] In mice, with the intracerebroventricular co-administration of a 50 µg dose of kelatorphan (this route is necessary because kelatorphan is incapable of crossing the blood-brain-barrier)[4] hence alongside exogenous [Met]enkephalin (ED50 approximately 10 ng), it potentiated the analgesic effects of the latter by 50,000 times.[1] Kelatorphan also displays potent antinociceptive effects alone,[5] and does not depress respiration, although at high doses it actually increases it.[4]
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