Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 1994 Nov 15;269(3):R1-2.
doi: 10.1016/0922-4106(94)90047-7.

Clozapine is a potent and selective muscarinic M4 receptor agonist

S H Zorn  1 , S B Jones, K M Ward, D R Liston
Affiliations

Clozapine is a potent and selective muscarinic M4 receptor agonist

S H Zorn et al. Eur J Pharmacol. .

Abstract

Clozapine was studied in functional assays at human muscarinic M1-M5 receptors expressed in Chinese hamster ovary cells. Clozapine was a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. In contrast, clozapine potently antagonized agonist-induced responses at the other four muscarinic receptor subtypes. Selective stimulation of M4 receptors may, in part, explain the hypersalivation observed clinically with clozapine. Moreover, the unique overall muscarinic profile of clozapine may contribute to its atypical antipsychotic efficacy.

PubMed Disclaimer

LinkOut - more resources