Clozapine N-oxide dihydrochloride
Clozapine N-oxide dihydrochloride用途
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 可特异性激活 DREADD 受体 hM3Dq。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。
Clozapine N-oxide dihydrochloride名称
Clozapine N-oxide dihydrochloride生物活性
[ 描述 ]:
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 可特异性激活 DREADD 受体 hM3Dq。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。
[ 相关类别 ]:
[ 靶点 ]
Human muscarinic designer receptors (DREADDs)[1]
[体外研究]
氯氮平N-氧化物(CNO)可以在恐惧激活所需的浓度下与非恐惧受体结合,并对其母体化合物氯氮平进行反向代谢,氯氮平是一种非典型抗精神病药,作用于多种药理靶点,产生多种生理和行为效应[2]。
[体内研究]
小鼠腹腔注射氯氮平氮氧化物(1 mg/kg)后,氯氮平氮氧化物(CNO)血浆浓度在15分钟达到峰值,2小时后非常低。尽管CNO在小鼠体内的半衰期很短,对表达恐惧的实验动物进行急性治疗后所描述的生物效应通常要长得多(6-10小时)[1]。
[参考文献]
[1]. Wess J, et al. Novel designer receptors to probe GPCR signaling and physiology. Trends Pharmacol Sci. 2013 Jul;34(7):385-92.
[2]. Manvich DF, et al. The DREADD agonist clozapine N-oxide (CNO) is reverse-metabolized to clozapine and produces clozapine-like interoceptive stimulus effects in rats and mice. Sci Rep. 2018 Mar 1;8(1):3840.
[3]. van der Peet PL, et al. Gram scale preparation of clozapine N-oxide (CNO), a synthetic small molecule actuator for muscarinic acetylcholine DREADDs. MethodsX. 2018 Mar 23;5:257-267.
[4]. Silva RR, et al. Evaluation of Functional Selectivity of Haloperidol, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine D2 Receptor. Front Pharmacol. 2019 Jun 4;10:628.
[5]. Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2.
Clozapine N-oxide dihydrochloride物理化学性质
[ 分子式 ]:
C18H21Cl3N4O
[ 分子量 ]:
415.74
[ 储存条件 ]:
2-8°C, 密封, 干燥
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