Drug intelligence / Profile preview

aconitine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Aconitine is a highly toxic diterpene alkaloid derived from plants of the *Aconitum* genus, such as *Aconitum napellus* (monkshood) and *Aconitum carmichaelii* (Fuzi). It is a potent neurotoxin and cardiotoxin that functions by binding with high affinity to Site 2 of voltage-gated sodium channels, preventing their inactivation and causing persistent depolarization of excitable membranes. This action results in severe arrhythmias, respiratory failure, and neurological symptoms. In Traditional Chinese Medicine (TCM), aconitine-containing preparations like 'Fuzi' are used for their analgesic and anti-inflammatory properties in treating rheumatoid arthritis and chronic pain, though they require rigorous processing (such as boiling) to hydrolyze aconitine into less toxic derivatives like benzoylaconine and aconine.

Other names
acetylbenzoylaconine
02

Targets

GYS1 (Glycogen synthase 1)NaV (Voltage-gated sodium channels)PLA2G4A (Cytosolic phospholipase A2 alpha)

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