The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Jan. 28, 1997
Filed:
Apr. 30, 1992
Kenneth Shaw, Weston, CT (US);
Alan Hutchison, Madison, CT (US);
Andrew Thurkauf, Branford, CT (US);
John Tallman, Guilford, CT (US);
Neurogen Corporation, Branford, CT (US);
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.