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Clozapine

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Chemical Structure| 5786-21-0 同义名 : HF 1854;LX 100-129;Clozapine (CRM)
CAS号 : 5786-21-0
货号 : A592547
分子式 : C18H19ClN4
纯度 : 98%
分子量 : 326.823
MDL号 : MFCD00153785
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(152.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • 5-HT2
描述 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[3]. The chemical structure of clozapine facilitates a relatively rapid dissociation from D2 receptors. Clozapine is very potent at D2 receptor with a Ki of 75 nM. Clozapine is also potent at the α2-adrenoceptor with a Ki value of 51 nM[4]. Mice were treated chronically (21 days) with 25 mg/kg/day clozapine. Head-twitch response was decreased and [(3)H]ketanserin binding was downregulated in 1, 7, and 14 days after chronic clozapine. 5-HT ( 2A ) mRNA was reduced 1 day after chronic clozapine[5]. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine can lower the seizure threshold in a dose- and time-dependent manner. Careful patient selection and monitoring are required when clozapine therapy is used in patients with schizophrenia[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00031317 Panic Disorder Phase 4 Completed - United States, Maryland ... 展开 >> National Institute of Mental Health (NIMH) Bethesda, Maryland, United States, 20892 收起 <<
NCT02949752 Antipsychotics Weight Gain Phase 4 Recruiting August 2017 Singapore ... 展开 >> Institute of Mental Health Recruiting Singapore, Singapore, 556121 Contact: Bee Choo Lim    63892000 ext 3618    Bee_Choo_LIM@imh.com.sg    Contact: Jaclyn Ong    63892000 ext 2959    jaclyn_yy_ong@imh.com.sg 收起 <<
NCT02926976 Schizophrenia Not Applicable Recruiting September 2018 China ... 展开 >> DTliu Recruiting Shanghai, China Contact: DT Liu, PHD       erliu110@126.com 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.30mL

3.06mL

1.53mL

30.60mL

6.12mL

3.06mL
参考文献

[1]Seeman P. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.

[2]Nguyen TV, Kosofsky BE, et al. Differential expression of c-fos and zif268 in rat striatum after haloperidol, clozapine, and amphetamine. Proc Natl Acad Sci U S A. 1992 May 15;89(10):4270-4.

[3]Zorn SH, Jones SB, Ward KM, Liston DR. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2

[4]Seeman P. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9

[5]Moreno JL, Holloway T, Umali A, Rayannavar V, Sealfon SC, González-Maeso J. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26

[6]Jann MW, Grimsley SR, Gray EC, Chang WH. Pharmacokinetics and pharmacodynamics of clozapine. Clin Pharmacokinet. 1993 Feb;24(2):161-76