For research use only. Not for therapeutic Use.
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].
| Catalog Number | I021477 |
| CAS Number | 1398496-82-6 |
| Synonyms | 5-(4-fluoro-1-benzothiophen-2-yl)-8-methyl-1,9-dihydro-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one |
| Molecular Formula | C19H12FN3O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C19H12FN3O2S/c1-9-5-10-6-14-15(25-19(24)21-14)7-11(10)18(23-22-9)17-8-12-13(20)3-2-4-16(12)26-17/h2-4,6-8H,5H2,1H3,(H,21,24) |
| InChIKey | WNUWGRVHGICCLS-UHFFFAOYSA-N |
| SMILES | CC1=NN=C(C2=CC3=C(C=C2C1)NC(=O)O3)C4=CC5=C(C=CC=C5S4)F |
| Reference | [1]. Etherington LA, et al. Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. Neuropharmacology. 2017;125:353-364. |
