| 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: |
-80℃(运输条件:冰袋低温运输) |
| 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 |
|
| 注意: |
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