Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
XB-ART-4282
J Med Chem 2003 Dec 18;4626:5567-70. doi: 10.1021/jm034164c.
Show Gene links Show Anatomy links

Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.

Li X , Cao H , Zhang C , Furtmueller R , Fuchs K , Huck S , Sieghart W , Deschamps J , Cook JM .


???displayArticle.abstract???
The synthesis and in vitro affinity of the alpha5beta3gamma2 (alpha5) subtype selective BzR/GABA(A) antagonist 7 is described. This ligand is selective for alpha5 subtypes in vitro and is a potent antagonist of the effects of diazepam only at alpha5beta3gamma2 subtypes (oocytes). Ligands such as 7 will be important in the determination of which physiological function(s) are subserved by this GABA(A) alpha5 subtype.

???displayArticle.pubmedLink??? 14667209
???displayArticle.link??? J Med Chem
???displayArticle.grants??? [+]

Species referenced: Xenopus
Genes referenced: bag3