Kelatorphan

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Kelatorphan
Kelatorphan.svg
Systematic (IUPAC) name
N-[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]-L-alanine
Clinical data
Legal status
  • Non-regulated
Identifiers
CAS Number 92175-57-0
ATC code None
PubChem CID: 123982
DrugBank DB08040
ChemSpider 110501
Chemical data
Formula C14H18N2O5
Molecular mass 294.303 g/mol
  • O=C(O)[C@@H](NC(=O)[C@H](Cc1ccccc1)CC(=O)NO)C
  • InChI=1S/C14H18N2O5/c1-9(14(19)20)15-13(18)11(8-12(17)16-21)7-10-5-3-2-4-6-10/h2-6,9,11,21H,7-8H2,1H3,(H,15,18)(H,16,17)(H,19,20)/t9-,11+/m0/s1
  • Key:OJCFZTVYDSKXNM-GXSJLCMTSA-N

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]

See also

References

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  4. ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'strict' not found.
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