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Formula | C14H18N2O5 |
Molar mass | 294.307 g·mol−1 |
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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]
Clinical data | |
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ATC code |
|
Legal status | |
Legal status |
|
Identifiers | |
| |
CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C14H18N2O5 |
Molar mass | 294.307 g·mol−1 |
3D model ( JSmol) | |
| |
|
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]