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Hydroxytacrine is a major active metabolite of tacrine (Item No. 70240).1 It is formed via hydroxylation of tacrine by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1A2. Hydroxytacrine inhibits acetylcholinesterase (AChE; IC50 = 4.8 µM).2 In vivo, hydroxytacrine (33 mg/kg) reverses scopolamine-induced memory impairment in mice without inducing acute toxicity.
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1. Inhibition of murine cytochrome P4501A by tacrine: In vitro studies. Drug Metab. Dispos. 32(8), 805-812 (2004).
2. (±)9-