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1-羟基咪达唑仑

1-羟基咪达唑仑用途

1'-Hydroxymidazolam 是 Midazolam 的主要活性代谢产物,并且是一种神经元抑制剂。1'-Hydroxymidazolam 能够抑制神经元活性并增加 Midazolam 的作用。

1-羟基咪达唑仑名称

[ CAS 号 ]:
59468-90-5

[ 中文名 ]:
1-羟基咪达唑仑

[ 英文名 ]:
1'-Hydroxymidazolam

[英文别名 ]:

1'-Hydroxymidazolam

1-羟基咪达唑仑生物活性

[ 描述 ]:

1'-Hydroxymidazolam 是 Midazolam 的主要活性代谢产物,并且是一种神经元抑制剂。1'-Hydroxymidazolam 能够抑制神经元活性并增加 Midazolam 的作用。

[ 相关类别 ]:

研究领域 >> 神经疾病

[体外研究]

1’-羟基咪唑安定(5 nM-1 M)在100 nM或更高浓度下诱导对动作电位放电速率的显著抑制,并且在野生型小鼠的新皮层切片培养中,随着浓度增加到1µM,网络活动抑制持续增加[2]。

[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.

1-羟基咪达唑仑物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
540.6±60.0 °C at 760 mmHg

[ 熔点 ]:
264-266ºC

[ 分子式 ]:
C₁₈H₁₃ClFN₃O

[ 分子量 ]:
341.767

[ 闪点 ]:
280.7±32.9 °C

[ 精确质量 ]:
341.073120

[ PSA ]:
50.41000

[ LogP ]:
3.14

[ 外观性状 ]:
白色或灰白色

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.687

[ 储存条件 ]:
2-8°C

1-羟基咪达唑仑MSDS

1-羟基咪达唑仑安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
11-23/24/25-39/23/24/25

[ 安全声明 (欧洲) ]:
7-16-36/37-45

[ 危险品运输编码 ]:
UN1230 - class 3 - PG 2 - Methanol, solution

[ WGK德国 ]:
3

1-羟基咪达唑仑合成路线

1-羟基咪达唑仑上下游产品

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1-羟基咪达唑仑文献

A comparison of the metabolism of midazolam in C57BL/6J and hepatic reductase null (HRN) mice.

Biochem. Pharmacol. 92(4) , 701-11, (2014)

The hepatic cytochrome P450 reductase null (HRN) mouse, which has no functional hepatic Cyp P450s, may represent a useful model for examining extra-hepatic P450-related oxidative metabolism. Here the ...

A highly sensitive liquid chromatography tandem mass spectrometry method for simultaneous quantification of midazolam, 1'-hydroxymidazolam and 4-hydroxymidazolam in human plasma.

Biomed. Chromatogr. 25(10) , 1091-8, (2011)

A highly sensitive liquid chromatography-tandem mass spectrometry method for the simultaneous quantification of midazolam and its major metabolites 1'-hydroxymidazolam and 4-hydroxymidazolam in human ...

Evidence of CYP3A allosterism in vivo: analysis of interaction between fluconazole and midazolam.

Clin. Pharmacol. Ther. 91(3) , 442-9, (2012)

The allosteric effect of fluconazole (effector) on the formation of 1'-hydroxymidazolam (1'-OH-MDZ) and 4-hydroxymidazolam (4-OH-MDZ) from midazolam (MDZ), a substrate of CYP3A4/5--members of the cyto...

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