U 93631 是一种新型化学结构的 GABAA 受体配体，IC50 为 100 nM，已显示可诱导重组 GABAA 受体中 GABA 诱导的全细胞 Cl 电流快速、时间依赖性衰减。
| Cas No. | 152273-12-6 |
| 化学名 | tert-butyl 4,4-dimethyl-4,5-dihydroimidazo[1,5-a]quinoxaline-3-carboxylate |
| Canonical SMILES | O=C(C(N=C1)=C2N1C3=CC=CC=C3NC2(C)C)OC(C)(C)C |
| 分子式 | C17H21N3O2 |
| 分子量 | 299.37 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. target: GABAA receptorIC 50: GABAA receptor[1]In vitro: 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. [1] References:
[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 |
