Novel gabaa receptor subtypes and methods for screening drug...

Details Novel gabaa receptor subtypes and methods for screening drug... Novel gabaa receptor subtypes and methods for screening drug...

C - Chemistry, Metallurgy

07

K

C07K 14/705 (2006.01) C07B 59/00 (2006.01) C07D 487/04 (2006.01) G01N 33/566 (2006.01) G01N 33/94 (2006.01)

Patent

CA 2134227

ABSTRACT OF THE DISCLOSURE The present invention provides methods for screening drug compounds utilizing compounds of formulas (I and II), and the pharmaceutically acceptable salts thereof where: R1, R2, R3, and R4 represent hydrogen, halogen, alkyl or alkoxy substituents; R5 is hydrogen or lower alkyl; X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; and Z is hydrogen or fluorine. The invention also provides tritium or iodine isotope radiolabeled compounds of the formulas (I and II) radiolabeled with tritium or isotopes of iodine. The invention further provides novel GABAa receptor subtypes which specifically bind to compounds of formulas (I or II). The invention also provides GABAa receptor subtypes which are bound in situ to a compound of formula (I or II). The compounds provided herein bind selectively to a novel subtype of the GABAa binding site. Selective interaction of ligands at this unique receptor population results in pharmacological specificity which may lead to superior anxiolytics, cognition enhancers, anticonvulsants and sedative hypnotics.

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