کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369984 981799 2012 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
A novel series of benzimidazole NR2B-selective NMDA receptor antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
A novel series of benzimidazole NR2B-selective NMDA receptor antagonists
چکیده انگلیسی

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 FLIPR-Ca2+ 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.

Discovery of a novel series of benzimidazole-derived NR2B selective NMDA receptor antagonists is described.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 7, 1 April 2012, Pages 2620–2623
نویسندگان
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