Afizagabar

小分子

阿菲扎加巴尔

Afizagabar

A656382-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR , with an IC 50 of 585 nM for α5β2γ2 and a K i of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy. In Vitro Afizagabar (S44819) is a competitive α5-GABAAR antagonist (K b =221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague Dawley (SPRD) rats (In the eight-arm radial maze) Dosage: 1 and 3 mg/kg Administration: I.p. Result: Significantly diminished the marked increase in total errors induced by Scopolamine.

Afizagabar (S44819) 是α5-GABAAR GABA 结合位点上的第一类竞争性和选择性拮抗剂，对 α5β2γ2 的 IC 50 为 585 nM，对 α5β3γ2 的 K i 为 66 nM。阿非扎巴能增强海马突触的可塑性，其 p

1398496-82-6(DMSO)

C19H12FN3O2S

365.38 g/mol

CC1=NN=C(C2=CC3=C(C=C2C1)NC(=O)O3)C4=CC5=C(C=CC=C5S4)F