Drug intelligence / Profile preview

benperidol

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

Overview

Benperidol is a highly potent first-generation (typical) antipsychotic of the butyrophenone class, primarily used for the treatment of schizophrenia, psychoses, manic episodes, and psychomotor agitation. It was discovered at Janssen Pharmaceutica in 1961 and has been marketed since 1966. Benperidol is considered the most potent neuroleptic on the European market, with a potency approximately eight times higher than haloperidol and up to one hundred times that of chlorpromazine. Its primary mechanism of action is strong antagonism at dopamine D2 receptor in the brain, which accounts for its antipsychotic effects; it also exhibits weaker antagonism at serotonin 5-HT2A receptor and minimal activity at histamine H1 receptor, alpha1-adrenergic receptor, muscarinic acetylcholine receptors. Benperidol can be administered orally or by intramuscular injection and is associated with a high risk of extrapyramidal side effects due to its strong dopamine receptor blockade[2][3][4][5][7][8].

Brand names
Anquil
02

Targets

DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)mAChR (Muscarinic acetylcholine receptors)

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