Drug intelligence / Profile preview

spiperone

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Oral
01

Overview

Spiperone is a typical antipsychotic drug of the butyrophenone class, primarily used as a dopamine antagonist that binds to dopamine (notably D2) and serotonin (5HT2A) receptors. It is licensed for clinical use in Japan under the brand name Spiropitan for the treatment of schizophrenia[2][4]. Spiperone has also been widely used as a research chemical, particularly in neuropharmacology and imaging studies. Beyond its antipsychotic effects, it has been identified through compound screening as an activator of calcium-activated chloride channels (CaCCs), suggesting potential therapeutic applications in cystic fibrosis by stimulating chloride secretion independently of CFTR[5]. Recent preclinical studies have shown that spiperone can induce cell cycle arrest and apoptosis in colorectal cancer cells by disrupting intracellular calcium kinetics, inducing endoplasmic reticulum stress, and affecting lipid metabolism[6][8].

Brand names
Spiropitan
Other names
spiroperidolespiperona
02

Targets

CaCC (Calcium-activated chloride channel protein regulator 1)HTR2A (Serotonin receptor 5-HT2A)DRD2 (Dopamine D2 Receptor)

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