Cholesta-3,5-dien-7-one

一种氧固醇和GABAA受体的负变构调节剂；降低表达α1β1γ2或α4β3γ2亚基的GABAA受体的HEK细胞中GABA诱导电流（IC50分别为1.5和1µM）；降低小鼠DRG分离神经元中肽能和非肽能伤害感受器、C-LTMR和冷热传感器的GABA诱导去极化；在2、10和50mg/kg剂量下增加小鼠热板测试中伤害性行为的潜伏期。An oxysterol and a negative allosteric modulator of GABAA receptors; reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors (IC50s = 1.5 and 1 µM, respectively); reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse DRG neurons; increases latency to nocifensive behaviors in the hot plate test in mice at 2, 10, and 50 mg/kg.分子式C27H42O分子量382.6O=C1C=C2C=CCC[C@]2(C)[C@]3([H])[C@]1([H])[C@@](CC[C@]4([H])[C@@H](CCCC(C)C)C)([H])[C@]4(C)CC3