کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366556 981595 2007 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors
چکیده انگلیسی

A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were determined. In particular, a nitrile substituent at the C5 position of the indole ring gave potent SERT activity. The stereochemistry of the N,N-dimethylamine substituent was determined for the most potent indole cyclohexenylamine, 6a. The enantiomers of 6a were energy minimized and compared to other conformationally restricted SSRIs. Compound 6a was found to give a dose–response similar to the SSRI fluoxetine in microdialysis studies in rats.

A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were determined. In particular, compound 6a gave potent SERT activity. The enantiomers of 6a were energy minimized and compared to other known conformationally restricted SSRIs. Compound 6a was also found to give a dose–response similar to the SSRI fluoxetine in microdialysis studies in rats.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 11, 1 June 2007, Pages 3099–3104
نویسندگان
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