2711603-38-0

Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].

5-HT_2A Receptor: 4 nM (Ki); 5-HT₆ Receptor; 5-HT₇ Receptor; mAChR1: 9.5 nM (Ki); mAChR4: 11 nM (EC₅₀); α2-adrenergic receptor: 51 nM (Ki); D₂ Receptor: 75 nM (Ki)

[1] Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9. DOI:10.1021/cn400189s
[2] Zhukovskaya NL, et al. Clozapine downregulates 5-hydroxytryptamine6 (5-HT6) and upregulates 5-HT7 receptors in HeLa cells. Neurosci Lett. 2000 Jul 21;288(3):236-40. DOI:10.1016/s0304-3940(00)01225-8
[3] Moreno JL, et al. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26. DOI:10.1007/s00213-012-2809-7
[4] Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2. DOI:10.1016/0922-4106(94)90047-7