1370000-25-1Relevant 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.
, 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.
