The unique efficacy of clozapine is attributable to muscarinic receptor agonism - PubMed
6 hours ago
- #clozapine
- #muscarinic receptors
- #schizophrenia
- Clozapine is uniquely effective for treatment-resistant schizophrenia compared to other antipsychotics.
- Its superior efficacy is attributed to its agonistic action on muscarinic acetylcholine receptors, unlike other antipsychotics.
- A cholinergic mechanism is supported by clozapine’s distinct pharmacology and the development of new cholinergic-based antipsychotics.
- An alternative hypothesis involving α2 noradrenergic receptor antagonism is considered implausible due to lack of clinical antipsychotic effects from such antagonists.
- Clozapine combines low-potency dopamine D2 receptor binding with partial agonism at muscarinic M1 and M4 receptors, which may underlie its ideal antipsychotic properties.