| Identification | Back Directory | [Name]
4H-Imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, 8-ethynyl-6-(2-fluorophenyl)-, ethyl ester | [CAS]
612526-36-0 | [Synonyms]
JY-XHe-053
4H-Imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, 8-ethynyl-6-(2-fluorophenyl)-, ethyl ester | [Molecular Formula]
C22H16FN3O2 | [MOL File]
612526-36-0.mol | [Molecular Weight]
373.38 |
| Hazard Information | Back Directory | [Description]
JY-XHe-053 is a selective modulator of GABAA receptors containing the α5 subunit. | [Uses]
JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors[1][2]. | [References]
[1] Rivas FM, Stables JP, Murphree L, et al. Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.?J Med Chem. 2009;52(7):1795-1798. DOI:10.1021/jm801652d
[2] Savi? MM, Majumder S, Huang S, et al. Novel positive allosteric modulators of GABAA receptors: do subtle differences in activity at alpha1 plus alpha5 versus alpha2 plus alpha3 subunits account for dissimilarities in behavioral effects in rats?.?Prog Neuropsychopharmacol Biol Psychiatry. 2010;34(2):376-386. DOI:10.1016/j.pnpbp.2010.01.004 |
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