Pipamperone is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia. It was developed by Janssen Pharmaceutica in 1961 and started its first round of clinical... In an effort to improve haloperidol's pharmacological effects, Janssen discovered that pipamperone, an agent whose pharmacological profile was distinct from haloperidol and all other known antipsychotic drugs at this time, had significant anti-tryptamine activity.
- Mechanism
- Curator reviewed · 5 references
Pipamperone binds mainly to 5-HT2A receptors, with a nearly equal affinity to D4 receptors and a moderate affinity for 5-HT2C, D2, D3, 1- and 2B-adrenoceptors.
This drug is a selective 5-HT2A, D1 and D4 antagonist. Extrapyramidal adverse effects also appear to be limited in pipamperone treatment compared to traditional antipsychotic medications due to its high receptor selectivity.
Pipamperone has a 15-fold higher affinity for D4 than D2 receptors. It has been suggested that D4 receptors may play a role in the modulation of GABAergic neuronal activity by dopamine.
- Primary indication
- Treatment of chronic psychoses and states of aggressiveness of various origins.Curator reviewed
- Formula / weight
- C21H30FN3O2 · 375.488 g/mol (avg)
- Also known as
- Carpiperone · Floropipamide · Fluoropipamide
Resolves to
AXKPFOAXAHJUAG-UHFFFAOYSA-NSMILESNC(=O)C1(CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1)N1CCCCC1What you can answer from here — as of September 23, 2026
Which drugs share a target with Pipamperone, and which of those have an active Phase 3 trial?
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