کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1378725 982007 2005 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
2-(Arylmethyl)-3-substituted quinuclidines as selective α7 nicotinic receptor ligands
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
2-(Arylmethyl)-3-substituted quinuclidines as selective α7 nicotinic receptor ligands
چکیده انگلیسی

A series of 2-(arylmethyl)-3-substituted quinuclidines was developed as α7 neuronal nicotinic acetylcholine receptor (nAChR) agonists based on a putative pharmacophore model. The series is highly selective for the α7 over other nAChRs (e.g., the α4β2 of the CNS, and the muscle and ganglionic subtypes) and is functionally tunable at α7. One member of the series, (+)-N-(1-azabicyclo[2.2.2]oct-3-yl)benzo[b]furan-2-carboxamide (+)-8l), has potent agonistic activity for the α7 nAChR (EC50 = 33 nM, Imax = 1.0), at concentrations below those that result in desensitization.

A series of 2-(arylmethyl)-3-substituted quinuclidines was developed as α7 neuronal nicotinic acetylcholine receptor (nAChR) agonists based on a putative pharmacophore model.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 8, 15 April 2005, Pages 2073–2077
نویسندگان
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