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Bioorg Med Chem Lett. 2004 Apr 5;14(7):1679-82.

Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.

Author information

1
Department of Medicinal Chemistry, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. james_crawforth@merck.com

Abstract

A series of tricyclic pyridones has been evaluated as benzodiazepine site ligands with functional selectivity for the alpha(3) over the alpha(1) containing subtype of the human GABA(A) 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.

PMID:
15026049
DOI:
10.1016/j.bmcl.2004.01.057
[Indexed for MEDLINE]

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