Cas No.: | 152273-12-6 |
Synonyms: | U-93631; U 93631 |
SMILES: | O=C(C1=C2N(C=N1)C3=C(C=CC=C3)NC2(C)C)OC(C)(C)C |
Formula: | C17H21N3O2 |
M.Wt: | 299.37 |
Purity: | >98% |
Sotrage: | 4°C for 1 year, -20°C for more than 2 years |
Description: | 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 receptor |
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 |