Title of article
Tricyclic pyridones as functionally selective human GABAAα2/3 receptor-ion channel ligands
Author/Authors
James Crawforth، نويسنده , , John R. Atack، نويسنده , , Susan M. Cook، نويسنده , , Karl R. Gibson، نويسنده , , Alan Nadin، نويسنده , , Andrew P. Owens، نويسنده , , Andrew Pike، نويسنده , , Michael Rowley، نويسنده , , Alison J. Smith، نويسنده , , Bindi Sohal، نويسنده , , Francine Sternfeld، نويسنده , , Keith Wafford، نويسنده , , Leslie J. Street، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
1679
To page
1682
Abstract
A series of tricyclic pyridones has been evaluated as benzodiazepine site ligands with functional selectivity for the α3 over the α1 containing subtype of the human GABAA receptor ion channel. This investigation led to the identification of a high affinity, functionally selective, orally bioavailable benzodiazepine site ligand that demonstrated activity in rodent anxiolysis models and reduced sedation relative to diazepam.
Keywords
Tricyclic pyridones , fax: +44-1279-440187 , GABAA.* Corresponding author. Tel.: +44-1279-440436 , e-mail: james_crawforth@merck.com
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794259
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