612526-36-0
612526-36-0
Chemical Structure
JY-XHe-053
- CAS No.: 612526-36-0
- Formula:C22H16FN3O2
- Molecular Weight:373.38
IUPAC Name: ethyl 8-ethynyl-6-(2-fluorophenyl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate
InChIKey: DANIDPUWXPDMNG-UHFFFAOYSA-N
SMILES: O=C(OCC)C1=C2CN=C(C3=CC(C#C)=CC=C3N2C=N1)C4=CC=CC=C4F
Biological Activity: 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].
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JY-XHe-053 | 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. | |||||||||||||||||||||
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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. [Content Brief]
- [2]. Savić 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. [Content Brief]
Keywords
