Gabaa receptor subtypes and methods for screening drug compounds

Details Gabaa receptor subtypes and methods for screening drug compounds Gabaa receptor subtypes and methods for screening drug compounds

1992-04-30

1997-01-28

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544346, C07D48706, C07D48704, C07D48702

Patent

active

055979203

ABSTRACT:
The present invention provides methods for screening drug compounds utilizing compounds of formulas I and II, where formulas I and II are ##STR1## and the pharmaceutically acceptable salts thereof where: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 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.

REFERENCES:
patent: 5075304 (1991-12-01), Hansen et al.
patent: 5130430 (1992-07-01), Shaw
patent: 5185446 (1993-02-01), Shaw et al.
patent: 5326868 (1994-07-01), Thurkauf

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