Drug intelligence / Profile preview

pipamperone

Development stage
Phase 3
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Oral
01

Overview

Pipamperone is a typical antipsychotic of the butyrophenone family, developed by Janssen Pharmaceutica in the early 1960s for the treatment of schizophrenia. It is primarily used as an antipsychotic and sedative, with additional benefits in managing agitation and sleep disturbances. Its mechanism of action involves antagonism at several neurotransmitter receptors, most notably serotonin (5-hydroxytryptamine) receptors—especially 5‑HT2A—and dopamine receptors (D2, D3, D4), with higher selectivity for 5‑HT2A and D4 over D2. It also blocks α1‑adrenergic and α2‑adrenergic receptors. The drug has relatively weak neuroleptic activity compared to other typical antipsychotics due to its moderate dopamine antagonism but pronounced serotonergic antagonism. This pharmacological profile led some to consider pipamperone a forerunner or even an early example of atypical antipsychotics[1][3][4].

Brand names
DipiperonDipiperalPiperonilPiperonylPropitan
Other names
CarpiperoneFloropipamideFluoropipamidePipamperonaPipamperonumDipiperonePipaneperone
02

Targets

ADRA2B (α2B)DRD3 (Dopamine receptor D3)DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)DRD2 (Dopamine D2 Receptor)ADRA2A (α2A)ADRA1A (α1A)HTR2C (5-hydroxytryptamine 2C receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)

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