期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 6, 页码 1582-1585出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.12.027
关键词
imidazo[1,2-a]pyrazin-8-ones; imidazo[1,2-d][1,2,4]triazin-8-ones; imidazo[2,1-f][1,2,4]triazin-8-ones; GABA(A) agonists; functionally selective for GABA(A) alpha 2 and alpha 3; anxiolytic
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1, 2-d] [ 1, 2,4]triazin-8 -ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABA(A) agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABA(A) alpha 2 and alpha 3-subtypes and is anxiolytic in a conditioned animal model of anxiety with minimal sedation observed at full BZ binding site occupancy. (C) 2006 Elsevier Ltd. All rights reserved.
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