Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM[1].
Anisatin inhibits [3H]diazepam binding enhanced by either GABA or pentobarbital, without affecting the basal specific binding to rat brain membranes[1].
In mice, the LD50 reported for anisatin ranges from 0.76 to 1 mg/kg (po and ip)[1].
[1]. Ikeda T, et al. Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999;127(7):1567-1576.
[2]. Bao X, et al. Bioavailability and Pharmacokinetics of Anisatin in Mouse Blood by Ultra-Performance Liquid ChromatograpTandem Mass Spectrometry. Biomed Res Int. 2020;2020:8835447. Published 2020 Dec 23.