U93631 是一种具有新型化学结构的 GABAA 受体配体，IC50 为 100 nM，它在重组 GABAA 受体中诱导 GABA 诱导的全细胞 Cl 电流快速，这种效果随时间依赖性衰减。

GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.

In the presence of U93631 at 5 UM, the peak amplitude decreased as a function of GABA concentration, with the half-maximal inhibitory concentration being approximately 100 nM, which is close to the Kd for the high affinity GABA site(85 nM). It appears that the drug interacts with GABA-bound receptors (at least monoliganded) and accelerates receptor desensitization, rather than acting as an open channel blocker.

152273-12-6

C17H21N3O2

299.374

DMSO:34 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years