The mechanism of action of clozapine

J Psychopharmacol. 2025 Apr;39(4):297-300. doi: 10.1177/02698811251319458. Epub 2025 Feb 13.

Abstract

Previous hypotheses for the superiority of clozapine over other antipsychotics have failed to stand the test of time. Here we describe how the unique pharmacology of clozapine in the peripheral nervous system held clues for solving the puzzle of clozapine in the central nervous system. Clozapine appears to have been the prototype for a new class of antipsychotics, now entering clinical psychiatry, which activates muscarinic acetylcholine receptors.

Keywords: Cobenfy; KarXT; M1; M4; Schizophrenia; acetylcholine; agonist; cholinergic; clozapine; emraclidine; mechanism; muscarinic; psychosis; receptor; striatum; xanomeline.

MeSH terms

  • Animals
  • Antipsychotic Agents* / pharmacology
  • Antipsychotic Agents* / therapeutic use
  • Central Nervous System / drug effects
  • Central Nervous System / metabolism
  • Clozapine* / pharmacology
  • Clozapine* / therapeutic use
  • Humans
  • Receptors, Muscarinic / drug effects
  • Receptors, Muscarinic / metabolism

Substances

  • Antipsychotic Agents
  • Clozapine
  • Receptors, Muscarinic