Minted: - / 5000

3069 Kelatorphan
3908d4d33d292bc127a30aa4361482c3ca678fd0bc6e18984e9f36b3926ab603

Properties

Background

Red
Bottle

Light blue
Cap

Red
Syringe

Yellow
Bubbles
No
Drops
No
Label
Bacterium

Chemistry

Formula
C14H18N2O5
Carbon
14
Polarity
Neutral

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). 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) hence alongside exogenous [Met]enkephalin (ED₅₀ approximately 10 ng), it potentiated the analgesic effects of the latter by 50,000 times. Kelatorphan also displays potent antinociceptive effects alone, and does not depress respiration, although at high doses it actually increases it.

From Wikipedia, the free encyclopedia. License: CC BY-SA.