کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1375463 981939 2005 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes
چکیده انگلیسی

A series of new 3-aryl-tropanes have been synthesized, and their affinities and selectivities were evaluated for monoamine transporters. (1RS)-3-(Fluoren-2-yl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene exhibited the highest affinity for the human serotonin transporter (IC50 = 14.5 nM). It is also 52-fold and 230-fold selective over human dopamine and norepinephrine transporters, respectively.

A 3-aryl-trop-2-ene ligand shown in the tentative binding pocket of a human monamine transporter. Conformational states A–D are dependent on the selection of the aromatic substituent at C3. The red colored electrostatic potential maps reveal the electron rich regions of A–D.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 24, 15 December 2005, Pages 5488–5493
نویسندگان
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