Afizagabar (Synonyms: S44819; Egis-13529) |
| رقم الكتالوجGC62829 |
Afizagabar (S44819) هو مضاد انتقائي وتنافسي من الدرجة الأولى في موقع ربط GABA لـ α5-GABAAR ، مع IC50 من 585 نانومتر لـ α5β2γ2 و Ki من 66 نانومتر لـ α5β3γ2
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Cas No.: 1398496-82-6
Sample solution is provided at 25 µL, 10mM.
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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.
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