کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10587591 981431 2013 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and binding affinity of new 1,4-disubstituted triazoles as potential dopamine D3 receptor ligands
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and binding affinity of new 1,4-disubstituted triazoles as potential dopamine D3 receptor ligands
چکیده انگلیسی
A series of new 1,4-disubstituted triazoles was prepared from appropriate arylacetylenes and aminoalkylazides using click chemistry methodology. These compounds were evaluated as potential ligands on several subtypes of dopamine receptors in in vitro competition assays, showing high affinity for dopamine D3 receptors, lower affinity for D2 and D4, and no affinity for the D1 receptors. Compound 18 displayed the highest affinity at the D3 receptor with a Ki value of 2.7 nM, selectivity over D2 (70-fold) and D4 (200-fold), and behaviour as a competitive antagonist in the low nanomolar range.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 20, 15 October 2013, Pages 5586-5591
نویسندگان
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