U93631

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Chemical Structure| 152273-12-6 同义名 : -
CAS号 : 152273-12-6
货号 : A112278
分子式 : C17H21N3O2
纯度 : 99%+
分子量 : 299.37
MDL号 : MFCD10566712
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors. In the presence of U-93631 at 5 microM, 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). The binding site for U-93631 on GABAA receptors seems not to overlap with GABA, barbiturate, or benzodiazepine sites, because the drug effect persisted in the presence of excess ligands for those sites. With cloned GABAA receptors composed of only alpha 1 beta 2, beta 2 gamma 2, or alpha 1 gamma 2 subunits, U-93631 also accelerated the decay rate[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.34mL

0.67mL

0.33mL

16.70mL

3.34mL

1.67mL

33.40mL

6.68mL

3.34mL

参考文献

[1]Dillon GH, Im WB, et al. [4-Dimethyl-3-t-butylcarboxyl-4,5-dihydro (1,5-a) quinoxaline] is a novel ligand to the picrotoxin site on GABAA receptors, and decreases single-channel open probability. J Pharmacol Exp Ther. 1995 Feb;272(2):597-603.

[2]Dillon GH, Im HK, et al. U-93631 causes rapid decay of gamma-aminobutyric acid-induced chloride currents in recombinant rat gamma-aminobutyric acid type A receptors. Mol Pharmacol. 1993 Oct;44(4):860-5.

[3]Dillon GH, Im HK, Hamilton BJ, Carter DB, Gammill RB, Judge TM, Im WB. U-93631 causes rapid decay of gamma-aminobutyric acid-induced chloride currents in recombinant rat gamma-aminobutyric acid type A receptors. Mol Pharmacol. 1993 Oct;44(4):860-5