A novel series of benzimidazole NR2B-selective NMDA receptor antagonists

…, C Virginio, L Abberley, P Goldsmith, AD Michel…

Index: Davies, David J.; Crowe, Matthew; Lucas, Nolwenn; Quinn, Joanna; Miller, David D.; Pritchard, Sara; Grose, David; Bettini, Ezio; Calcinaghi, Novella; Virginio, Caterina; Abberley, Lee; Goldsmith, Paul; Michel, Anton D.; Chessell, Iain P.; Kew, James N.C.; Miller, Neil D.; Gunthorpe, Martin J. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2620 - 2623

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Citation Number: 8

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 (pIC50> 7) and good selectivity against the NR2A subunit (pIC50< 4.3) as defined by ...

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