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- 产品描述: 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.
- 靶点: GABA Receptor;GABAReceptor
- 体外研究:
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.
- 参考文献:
1. Dillon,GH et al.U-93631 causes rapid decay of gamma-aminobutyric acid-induced chloride currents in recombinant rat gamma-aminobutyric acid type A receptors.Molecular Pharmacology October 1993, 44 (4) 860-865
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.34 ml 16.702 ml 33.404 ml 5 mM 0.668 ml 3.34 ml 6.681 ml 10 mM 0.334 ml 1.67 ml 3.34 ml 50 mM 0.067 ml 0.334 ml 0.668 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)