A New Pyridazine Series of GABA sub(A) alpha 5 Ligands

Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABA sub(A) receptors. The structural novelty of 6, compared to our advanced series of GABA sub(A) alpha 5 inverse agonists, made it an attractive molecule for further...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2005-09, Vol.48 (19), p.6004-6011
Main Authors: van Niel, MB, Wilson, K, Adkins, CH, Atack, J R, Castro, J L, Clarke, DE, Fletcher, S, Gerhard, U, Mackey, M M, Malpas, S, Maubach, K, Newman, R, O'Connor, D, Pillai, G V
Format: Article
Language:English
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Summary:Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABA sub(A) receptors. The structural novelty of 6, compared to our advanced series of GABA sub(A) alpha 5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABA sub(A) alpha 5 receptor subtypes.
ISSN:0022-2623
DOI:10.1021/jm050249x