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2250025-93-3

中文名称 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
英文名称 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
CAS 2250025-93-3
分子式 C18H21Cl3N4O-
分子量 415.745
MOL 文件 2250025-93-3.mol
更新日期 2024/07/12 22:11:58
2250025-93-3 结构式 2250025-93-3 结构式

基本信息

中文别名
氯氮平N-氧化盐酸
英文别名
Clozapine N-oxide dihydrochloride
Clozapine N-oxide dihydrochloride salt
8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride

物理化学性质

储存条件Store at 4°C,stored under nitrogen
溶解度溶于二甲基亚砜
形态结晶固体
颜色橙色
水溶解性Soluble in water (100 mM). Always store solutions at -20°C.

常见问题列表

生物活性
Clozapine N-oxide dihydrochloride 是一种 Clozapine 的主要代谢产物,也是一种人毒蕈碱设计受体 (DREADDs) 激动剂。Clozapine N-oxide dihydrochloride 可激活 DREADD 受体 hM3Dq 和 hM4Di。Clozapine N-oxide dihydrochloride 可以穿过血脑屏障。Clozapine 是一种有效的多巴胺拮抗剂,也一种是有效的选择性毒蕈碱 M4 受体 (muscarinic M4 receptor) (EC50 为 11 nM) 激动剂。
靶点

Human muscarinic designer receptors (DREADDs)

体外研究

Clozapine N-oxide (CNO) can bind to non-DREADD receptors at concentrations required for DREADD activation, and undergoes reverse-metabolism to its parent compound clozapine, an atypical antipsychotic that acts at a variety of pharmacological targets and produces numerous physiological and behavioral effects.

体内研究

After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h).

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