Drug intelligence / Profile preview

ritanserin

Development stage
Phase 2
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Oral
01

Overview

Ritanserin is a potent and selective serotonin (5-hydroxytryptamine, 5-HT) receptor antagonist, primarily targeting the 5-HT2A and 5-HT2C subtypes with high affinity. It also exhibits antagonistic activity at other serotonin receptors including 5-HT1D, 5-HT2B, 5-HT5A, 5-HT6, and 5-HT7 but has much lower affinity for histaminergic (H1), dopaminergic (D2), and adrenergic (α1 and α2) receptors. Developed originally by Janssen as an investigational drug for psychiatric disorders such as anxiety, depression, schizophrenia, and cocaine-related disorders, ritanserin was never approved or marketed for clinical use. Its mechanism of action involves blocking the effects of serotonin at the targeted receptors in the central nervous system. Ritanserin is classified chemically as a piperidine-pyrimidinone derivative[1][3][4][5].

Other names
ritanserina
02

Targets

ADRA1A (α1A)RAF1 (c-Raf-1 (Y340D/Y341D))HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))DGKA (Diacylglycerol kinase alpha)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)DRD2 (Dopamine D2 Receptor)ADRA2A (α2A)HRH1 (Histamine H1 Receptor)

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