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α-Santalol is a naturally occurring sesquiterpene and the primary active constituent of East Indian sandalwood oil (*Santalum album*). It has been extensively investigated for its chemopreventive, anti-inflammatory, antimicrobial, and neuroleptic properties. In oncology models, α-santalol exhibits potent antimitotic and pro-apoptotic activities by directly binding to tubulin at the colchicine site, thereby inhibiting microtubule polymerization and inducing G2/M cell cycle arrest. It also acts as an antagonist of vascular endothelial growth factor receptor 2 (VEGFR2) to suppress angiogenesis, and has been identified as a cannabinoid receptor 2 (CB2) agonist. Additionally, α-santalol exhibits weak antagonistic activity against dopamine D2 and serotonin 5-HT2A receptors, contributing to its observed sedative and neuroleptic effects. It has been clinically evaluated in topical formulations for the treatment of skin conditions, including common warts and molluscum contagiosum.
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