Ajmalicine

alkaloid · nervous · cardiovascular · Oral

Ajmalicine, an alkaloid. A corynanthe-type indole alkaloid present in yohimbe bark (Pausinystalia johimbe) that shares the pentacyclic indole core of yohimbine.…

A corynanthe-type indole alkaloid present in yohimbe bark (Pausinystalia johimbe) that shares the pentacyclic indole core of yohimbine. Functional studies in pithed rats show it acts as a preferential α₁-adrenoceptor antagonist (PMID:3021076). Marketed elsewhere (as raubasine) as a cerebral vasodilator; quantitative human receptor pharmacology and clinical PK are not characterised. It is also a potent inhibitor of human CYP2D6 (Ki ≈ 3.3 nM; GtoPdb, PMID:8487254), a potential basis for pharmacokinetic interactions.

PubChem CID 441975 (C21H24N2O3, MW 352.4). Present in yohimbe bark: PMID:23657953 (UPLC-IM-QTOF profile; "yohimbine or ajmalicine core structure") + PMID:25905738. INTERACTIONS: ACQUITTED — THIS IS EXACTLY WHAT THE FIELD WAS DESIGNED FOR. All eight edges carry the same value because they cite the same measurement, "a potent in-vitro CYP2D6 inhibitor (Ki 3.3 nM)", and a Ki belongs to an ENZYME rather than to a victim, so one CYP2D6 constant legitimately applies to every CYP2D6 substrate. The repetition that made an automated screen flag this block is correct pharmacology, not a template. The basis is now declared explicitly so the next screen does not have to rediscover it. THE RECORD OWN CAVEAT STANDS AND IS THE RIGHT ONE: this is in-vitro potency, and whether ajmalicine ever reaches an inhibitory concentration in humans is a separate question the edges do not answer.

Related compounds

Sources: PMID:23657953, PMID:3021076, PMID:25905738, PMID:8487254