| Bioactivity | Clozapine (HF 1854) 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]. | ||||||||||||
| Invitro | Clozapine (HF 1854) is a D2 receptor antagonist with a Ki of 75 nM, blocks the serotonin 5HT2A receptor with a Ki of 4 nM, inhibits the muscarinic M1 receptor with a Ki of 9.5 nM, blocks α2-adrenoceptor with a Ki value of 51 nM[1].Clozapine (0-1 μM; 24 h) downregulates 5-HT6 and upregulates 5-HT7 receptors in HeLa cells[2].Clozapine is a full agonist at the muscarinic M4 receptor (EC50=11 nM) expressed in CHO cells[4]. | ||||||||||||
| In Vivo | Clozapine (HF 1854) (25 mg/kg/day; i.p.; 21 days) shows antipsychotic effects in lysergic acid diethylamide-induced psychosis mouse model[3]. Animal Model: | ||||||||||||
| Name | Clozapine | ||||||||||||
| CAS | 5786-21-0 | ||||||||||||
| Formula | C18H19ClN4 | ||||||||||||
| Molar Mass | 326.82 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9. [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. [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. [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. |