1'-Hydroxymidazolam | 咪达唑仑杂质1

MCE 国际站：1'-Hydroxymidazolam

中文名：咪达唑仑杂质1

CAS：59468-90-5

品牌：MedChemExpress (MCE)

存储条件：-20°C, stored under nitrogen

生物活性：1'-Hydroxymidazolam 是 Midazolam 的主要活性代谢物，是一种神经元抑制剂。 1'-羟基咪达唑仑可抑制神经元活动，增加了咪达唑仑的作用^[1][2]。

体外：1'-Hydroxymidazolam (5 nM-1 µM) 在浓度为 100 nM 或更高时显着抑制动作电位放电率，并随着新皮质切片中浓度增加至 1 µM 导致网络活动抑制稳步增加来自野生型小鼠的培养物^[2]。

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研究领域：Metabolic Enzyme/Protease

作用靶点：Drug Metabolite

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参考文献：[1]. Hasegawa T, et, al. Increase in the systemic exposure of primary metabolites of Midazolam in rat arising from CYP inhibition or hepatic dysfunction. Drug Metab Pharmacokinet. 2017 Feb; 32(1): 69-76.

[2]. Balk M, et, al. Differential depression of neuronal network activity by midazolam and its main metabolite 1-hydroxymidazolam in cultured neocortical slices. Sci Rep. 2017 Jun 14; 7(1): 3503.