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A Pyridazine Series of α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety

Lookup NU author(s): Dr Tim Blackburn


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The development of a series of GABAA α2/α3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably α3-selective compound ideal for in vivo study. These ligands are antagonists at the α1 subtype, with good CNS penetration and receptor occupancy, and excellent oral bioavailability.

Publication metadata

Author(s): Lewis R, Blackaby W, Blackburn T, Jennings A, Pike A, Wilson R, Hallet D, Cook S, Pushpinder F, Marshall G, Reynolds D, Sheppard W, Smith A, Sohal B, Stanley J, Tye S, Wafford K, Atack J

Publication type: Article

Publication status: Published

Journal: Journal of Medicinal Chemistry

Year: 2006

Volume: 49

Issue: 8

Pages: 2600-2610

Print publication date: 22/03/2006

ISSN (print): 0022-2623

ISSN (electronic): 1520-4804

Publisher: ACS Publications


DOI: 10.1021/jm051144x


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