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J Med Chem. 2006 Apr 20;49(8):2600-10.

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

Author information

1
The Neuroscience Research Centre, Merck Sharp & Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom. richard_t_lewis@btinternet.com

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.

PMID:
16610803
DOI:
10.1021/jm051144x
[Indexed for MEDLINE]

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