کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1358734 981359 2015 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold
چکیده انگلیسی

A series of compounds with quinazoline scaffold were designed, synthesized and evaluated as novel potent 5-HT2A receptor ligands. N-(4-Chlorophenyl)-2-(piperazin-1-yl)quinazolin-4-amine (5o) has a Ki value of 14.04 ± 0.21 nM, with a selectivity more than 10,000 fold over 5-HT1A receptors (D1 and D2-like receptors). The functional assay showed that this compound is an antagonist to 5-HT2A receptor with an IC50 value of 1.66 μM.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 18, 15 September 2015, Pages 3970–3974
نویسندگان
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