Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.
信号通路
GPCR & G Protein; Neuronal Signaling
靶点
5-HT2
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IC50
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体外研究
Clozapine and N-desmethylclozapine antagonized 5-HT-stimulated phosphoinositide hydrolysis with IC50 values of 110 and 29.4nM, respectively. Clozapine N-oxide was less potent.
体内研究
When administered clozapine, mean CNO plasma concentrations of 17.7 +/- 16.4ng/ml were slightly lower than the other clozapine metabolite-desmethylclozapine (DCLOZ) plasma levels of 24.4 +/- 8.6ng/ml at the 12 hour time point. When CNO was administered, plasma concentrations at the 12 hour time point of clozapine were twice the amount of CNO (28.1 +/- 8.9ng/ml vs 14.4 +/- 8.8ng/ml). Clozapine and its metabolite clozapine-N-oxide (0.5mg/kg) were administered intraperitoneally to guinea-pigs. Significant amounts of clozapine were detected in plasma, liver, frontal cortex and caudate after clozapine-N-oxide administration.
临床实验
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特征
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相关实验数据(此数据来自于公开文献,信裕生物并不保证其有效性):
酶活性检测实验
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细胞实验
细胞系
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浓度
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处理时间
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方法
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动物实验
动物模型
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配制
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剂量
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给药方式
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参考文献: 1. Kuoppamki M, et al. Eur J Pharmacol. 1993 Apr 15, 245(2), 179-82.
2. Chang WH, et al. Prog Neuropsychopharmacol Biol Psychiatry. 1998 Jul, 22(5), 723-39.
3. Jann MW, et al. Arch Int Pharmacodyn Ther. 1994 Sep-Oct, 328(2), 243-50.
包装清单: