| Literature DB >> 22366657 |
David J Davies1, Matthew Crowe, Nolwenn Lucas, Joanna Quinn, David D Miller, Sara Pritchard, David Grose, Ezio Bettini, Novella Calcinaghi, Caterina Virginio, Lee Abberley, Paul Goldsmith, Anton D Michel, Iain P Chessell, James N C Kew, Neil D Miller, Martin J Gunthorpe.
Abstract
A series of novel benzimidazoles are discussed as NR2B-selective N-methyl-d-aspartate (NMDA) receptor antagonists. High throughput screening (HTS) efforts identified a number of potent and selective NR2B antagonists such as 1. Exploration of the substituents around the core of this template identified a number of compounds with high potency for NR2B (pIC(50) >7) and good selectivity against the NR2A subunit (pIC(50) <4.3) as defined by FLIPR-Ca(2+) and radioligand binding studies. These agents offer potential for the development of therapeutics for a range of nervous system disorders including chronic pain, neurodegeneration, migraine and major depression.Entities:
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Year: 2012 PMID： 22366657 DOI： 10.1016/j.bmcl.2012.01.108
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823