کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10591276 | 981749 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of positron emission tomography radiotracers targeting serotonin 4 receptors in brain: [18F]MNI-698 and [18F]MNI-699
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Two new benzodioxane derivatives were synthesized as candidates to image the serotonin 4 receptors by positron emission tomography (PET) and radiolabeled with fluorine-18 via a two-step procedure. Competition binding assays demonstrated that MNI-698 and MNI-699 had sub-nanomolar binding affinities against rat striatal 5-HT4 receptors (Ki of 0.20 and 0.07Â nM, respectively). PET imaging in rhesus monkey showed that the regional brain distribution of [18F]MNI-698 and [18F]MNI-699 were consistent with the known densities of 5-HT4 in brain. [18F]MNI-698 and [18F]MNI-699 are among the first fluorine-18 radiotracers developed for imaging the 5-HT4 receptors in vivo and are currently under preclinical investigation in primates for future human use.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 23, 1 December 2013, Pages 6243-6247
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 23, 1 December 2013, Pages 6243-6247
نویسندگان
Fabien Caillé, Thomas J. Morley, Adriana Alexandre S. Tavares, Caroline Papin, Nicole M. Twardy, David Alagille, H. Sharon Lee, Ronald M. Baldwin, John P. Seibyl, Olivier Barret, Gilles D. Tamagnan,