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Etiocholanolone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Etiocholanolone图片
CAS NO:53-42-9
包装:5mg
市场价:540元

产品介绍
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。
Cas No.53-42-9
别名3a-羟基-5b-雄甾烷-17-酮,5β-Androsterone
Canonical SMILESC[C@@]1(CC2)[C@](CC3)([H])[C@](CC[C@]1([H])C[C@@H]2O)([H])[C@@](CCC4=O)([H])[C@]34C
分子式C19H30O2
分子量290.44
溶解度DMSO: 100 mg/mL (344.31 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].

Etiocholanolone (10 μM) coapplication with GABA leads to an increase in the relative frequency of long openings (fraction of OT3, site A2 effect), but it is ineffective at increasing the duration of long openings (site B effect) or at decreasing the relative frequency of the activation-related closed time component (site A1 effect)[2].

Etiocholanolone (intraperitoneal injection; 0-109.1 mg/kg; single dose) exhibits ED50 values of 57.6 and 109.1 mg/kg in the 6-Hz and PTZ tests, respectively. Protective activity in the 6-Hz test of 5β,3α-A persists for 2 h and is shorter than ent-5β,3α-A treatment (3 hours) in mice[1].

[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.