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/ 多巴胺受体 / Clozapine

氯氮平 /Clozapine {[allProObj[0].p_purity_real_show]}

货号：A592547 同义名： HF 1854;LX 100-129

Clozapine, an antipsychotic drug, is antagonist of dopamine and other receptors used to treat schizophrenia with a Ki value of 9.5 nM for M1 receptor.

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Clozapine 化学结构 CAS号：5786-21-0
Clozapine 化学结构
CAS号：5786-21-0
Clozapine 3D分子结构
CAS号：5786-21-0
Clozapine 化学结构 CAS号：5786-21-0
Clozapine 3D分子结构 CAS号：5786-21-0
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Clozapine 纯度/质量文件 产品仅供科研

货号：A592547 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 D1 receptor ↓ D2 receptor ↓ D3 receptor ↓ D4 receptor ↓ D5 receptor ↓ DAT ↓ Dopamine receptor ↓ 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

 		98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

 		98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 95%
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

 		98%
Levosulpiride ✔ 99+%
Pridopidine ✔ 95%
Metoclopramide ✔ ✔ 99+%
Molindone HCl ✔ 98%
Sulpiride ✔ 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		98+%
Phenothiazine ✔ 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

 		+++

Dopamine D2 receptor, Ki: 3.0 nM

 		++++

Dopamine D3 receptor, Ki: 0.83 nM

 		98%
Rotundine ++

D1 receptor, IC50: 166 nM

 		+

D2 receptor, IC50: 1.47 μM

 		+

D3 receptor, IC50: 3.25 μM

 		98%
Domperidone ✔ 99+%
ONC206 ✔ 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

 		++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

 		++++

D5 dopamine receptor, Ki: 0.3 nM

 		98%
MPP+ iodide ✔ 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

 		97%
Benztropine mesylate ++

DAT, IC50: 118 nM

 		98%
Azaperone ✔ 98%
Ziprasidone HCl ✔ 98+%
Paliperidone ✔ 98%
Alizapride HCl ✔ 99+%
Amisulpride ✔ 98%
Quetiapine hemifumarate ✔ Adrenergic Receptor 98%
Clozapine N-oxide ✔ 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Clozapine 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].

Clozapine 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 <<

Clozapine 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

Clozapine 实验方案

计算器
存储液制备 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

Clozapine 技术信息

CAS号5786-21-0
分子式C18H19ClN4
分子量 326.823
别名 HF 1854;LX 100-129;Clozapine (CRM)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

Tags: Clozapine | 5786-21-0 | HF 1854 | HF1854 | HF-1854 | Dopamine Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Dopamine Receptor | mAChR | Adrenergic Receptor | 5-HT Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Clozapine 纯度/质量文件 | Clozapine 亚型比较 | Clozapine 生物活性 | Clozapine 临床数据 | Clozapine 参考文献 | Clozapine 实验方案 | Clozapine 技术信息

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