Epipregnanolone 是一种天然存在的 5β-还原性神经甾体,是一种有效的电压依赖性 T 通道 (T-channels) 阻滞剂。Epipregnanolone 抑制 DRG T 电流,IC50 为 2 μM (at Vh of -90 mV)。Epipregnanolone 作为部分激动剂作用于鸟类中枢神经系统中 GABAA 受体复合物的共同神经甾体调节部位。
生物活性
Epipregnanolone, a naturally occurring 5β-reduced neurosteroid, is a potent, voltage-dependent blocker of T-channels. Epipregnanolone inhibits DRG T-currents with an IC 50 of 2 μM (at Vh of -90 mV). Epipregnanolone acts as a partial agonist on a common neurosteroid modulatory site of the GABA A receptor complex in avian CNS.
性状
Solid
IC50 & Target[1][2]
T-channels GABAA
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
结构分类
Steroids
参考文献
[1]. Ayoola C, et al. Inhibition of CaV3.2 T-type calcium channels in peripheral sensory neurons contributes to analgesic properties of epipregnanolone. Psychopharmacology (Berl). 2014;231(17):3503-3515.[2]. Pignataro L, et al. Epipregnanolone acts as a partial agonist on a common neurosteroid modulatory site of the GABA(A) receptor complex in avian CNS. Neurochem Res. 1997;22(2):221-225.