Afizagabar (S44819) 是一种首创的，有竞争性的，选择性的 α5-GABAAR 拮抗剂，对α5β2γ2 的IC50 值 585 nM，对 α5β3γ2 的 Ki 为 66 nM。Afizagabar 增强海马突触可塑性并显示促认知功效。
货号:ajcx34492
CAS:1398496-82-6
分子式:C19H12FN3O2S
分子量：365.38
溶解度:DMSO : 6.25 mg/mL (17.11 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy[1].

Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1].

Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1].

[1]. Etherington LA, et al. Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. Neuropharmacology. 2017;125:353-364.