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A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Authors :
Lewis RT
Blackaby WP
Blackburn T
Jennings AS
Pike A
Wilson RA
Hallett DJ
Cook SM
Ferris P
Marshall GR
Reynolds DS
Sheppard WF
Smith AJ
Sohal B
Stanley J
Tye SJ
Wafford KA
Atack JR
Source :
Journal of medicinal chemistry [J Med Chem] 2006 Apr 20; Vol. 49 (8), pp. 2600-10.
Publication Year :
2006

Abstract

The development of a series of GABA(A) alpha2/alpha3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably alpha3-selective compound ideal for in vivo study. These ligands are antagonists at the alpha1 subtype, with good CNS penetration and receptor occupancy, and excellent oral bioavailability.

Details

Language :
English
ISSN :
0022-2623
Volume :
49
Issue :
8
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
16610803
Full Text :
https://doi.org/10.1021/jm051144x