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3a-羟基-5b-雄甾烷-17-酮

3a-羟基-5b-雄甾烷-17-酮用途

Etiocholanolone (5β-Androsterone) 是睾酮的排泄代谢物,具有抗惊厥活性。相对于其对映体形式,Etiocholanolone 是一种较弱的神经甾醇类 GABAA receptor 正向变构调节剂。

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3a-羟基-5b-雄甾烷-17-酮名称

[ CAS 号 ]:
53-42-9

[ 中文名 ]:
还原胆烷醇酮

[ 英文名 ]:
Etiocholanolone

[中文别名 ]:

3a-羟基-5b-雄甾烷-17-酮

[英文别名 ]:

3a-Hydroxy-5b-androstane-17-one
Androsterone, (5β)-
3alpha-hydroxy-5beta-androstan-17-one
5β-Androsterone
(5b)-Androsterone
5-Isoandrosterone
3α-hydroxy-5β-androstane-17-one
5β-Androstan-17-one, 3α-hydroxy-
5BETA-ANDROSTERONE
MFCD00064133

3a-羟基-5b-雄甾烷-17-酮生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[体外研究]

乙酰胆醇酮(10μM)与GABA联合施用可导致长开口的相对频率增加(OT3的分数,A2位点效应),但对于增加长开口的持续时间(B位点效应)或降低激活相关闭合时间成分的相对频率(A1位点效应)[2]。

[体内研究]

在6-Hz和PTZ试验中,乙氧胆醇酮(腹腔注射；0-109.1mg/kg；单次剂量)的ED50值分别为57.6和109.1mg/kg。5β,3α-A在6-Hz试验中的保护作用持续2小时,比ent-5β,3α-A治疗(3小时)短[1]。

[参考文献]

[1]. Ping Li,et al. Natural and Enantiomeric Etiocholanolone Interact With Distinct Sites on the Rat alpha1beta2gamma2L GABAA Receptor. Mol Pharmacol. 2007 Jun;71(6):1582-90.

[2]. Dorota Zolkowska, et al. Anticonvulsant Potencies of the Enantiomers of the Neurosteroids Androsterone and Etiocholanolone Exceed Those of the Natural Forms. Psychopharmacology (Berl). 2014 Sep;231(17):3325-32.

3a-羟基-5b-雄甾烷-17-酮物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
413.1±45.0 °C at 760 mmHg

[ 熔点 ]:
148～150°C (lit.)

[ 分子式 ]:
C₁₉H₃₀O₂

[ 分子量 ]:
290.440

[ 闪点 ]:
176.4±21.3 °C

[ 精确质量 ]:
290.224579

[ PSA ]:
37.30000

[ LogP ]:
3.75

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.536

[ 储存条件 ]:
2-8°C

3a-羟基-5b-雄甾烷-17-酮MSDS

3a-羟基-5b-雄甾烷-17-酮安全信息

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

[ 危害码 (欧洲) ]:
F,Xn

[ 风险声明 (欧洲) ]:
11-20/21/22-36

[ 安全声明 (欧洲) ]:
16-36/37

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

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3a-羟基-5b-雄甾烷-17-酮文献

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Neurosteroid analogues. 12. Potent enhancement of GABA-mediated chloride currents at GABAA receptors by ent-androgens.

Eur. J. Med. Chem. 43 , 107-13, (2008)

Allopregnanolone (1) and pregnanolone (2), steroids containing a 17beta-acetyl group, are potent enhancers of GABA (gamma-aminobutyric acid) action at GABAA receptors. Their effects are enantioselecti...

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