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抑制剂描述:

产品名称:ClozapineN-Oxide

产品别名:见爱必信官网

英文别名:ClozapineN-Oxide

靶点:5-HT Receptor

CAS:34233-69-7

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Clozapine N-oxide 是 Clozapine 的惰性代谢物,Clozapine 是一种有效的 5-HT1C 受体拮抗剂。Clozapine N-oxide (CNO) 是一种 DREADD 激动剂。

溶解性:10 mM in DMSO

体外研究:

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. Acutely administered CNO can be metabolically converted to Clozapine in other species such as human and guinea-pig. The metabolites that may form after chronic administration of CNO to DREADD-expressing mice (or other species) have not been studied systematically. However, even if back-transformation to Clozapine occurs after chronic CNO administration, it should be noted that Clozapine is a more potent (by ~10-fold) DREADD agonist than CNO itself. Moreover, confounding biological effects of potential CNO metabolites can be easily identified by including both saline- and CNO-treated WT animals in a particular DREADD study. 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). One possibility is that CNO tends to accumulate in tissues, although other scenarios are also feasible. Using a general pharmacokinetic model for the interconversion process, the mean total clearances of Clozapine and Clozapine N-oxide (CNO) are 28.45 L/hr and 45.30 L/hr, respectively.

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