| Identification | Back Directory | [Name]
CLOZAPINE HYDROCHLORIDE | [CAS]
2711603-38-0 | [Synonyms]
CLOZAPINE HYDROCHLORIDE
8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine,dihydrochloride | [Molecular Formula]
C18H20Cl2N4 | [MDL Number]
MFCD06797816 | [MOL File]
2711603-38-0.mol | [Molecular Weight]
363.28 |
| Hazard Information | Back Directory | [Uses]
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]. | [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: | Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model[3]. | | Dosage: | 25 mg/kg/day. | | Administration: | Intraperitoneal injection, 21 days. | | Result: | Decreased head-twitch response, reduced 5-HT2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2. |
| [IC 50]
5-HT2A 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) | [References]
[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 |
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