1370000-28-4Relevant articles and documents
A novel series of benzimidazole NR2B-selective NMDA receptor antagonists
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.
scheme or table, p. 2620 - 2623 (2012/05/05)
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 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.
