Chlorpromazine is a phenothiazine that exhibits antipsychotic, antidepressant, anxiolytic, neuroprotective, and anticancer chemotherapeutic activities. Chlorpromazine inhibits D1/2/3/4 receptors, 5-HT1/2 receptors, α1/2-adrenergic receptors, and M1/2 muscarinic acetylcholine receptors (mAChRs). Chlorpromazine stabilizes misfolding motifs of prions, preventing oligomerization. Additionally, this compound acts as a functional inhibitor of acid sphingomyelinase (FIASMA). In vivo, chlorpromazine induces autophagy and apoptosis, inhibiting growth of glioma tumors.