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.
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Afizagabar
CAS number：1398496-82-6(DMSO) molecular formula：C19H12FN3O2S
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| Chinese alias | 阿菲扎加巴尔 | ||
| English alias | - | ||
| CAS number | 1398496-82-6(DMSO) | molecular formula | C19H12FN3O2S |
| molecular weight | 365.38 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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