کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370270 | 981814 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
Obesity remains a significant public health issue leading to Type II diabetes and cardiovascular disease. CB1 antagonists have been shown to suppress appetite and reduce body weight in animal models as well as in humans. Evaluation of pre-clinical CB1 antagonists to establish relationships between in vitro affinity and in vivo efficacy parameters are enhanced by ex vivo receptor occupancy data. Synthesis and biological evaluation of a novel and highly selective radiolabeled CB1 antagonist is described. The radioligand was used to conduct ex vivo receptor occupancy studies.
Ex vivo autoradiography of rat brain sagittal sections following drug treatment utilizing [3H]BMS-725519.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 22, 15 November 2011, Pages 6856–6860
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 22, 15 November 2011, Pages 6856–6860
نویسندگان
Yifan Yang, Keith J. Miller, Yeheng Zhu, Yang Hong, Yuan Tian, Natesan Murugesan, Zhengxiang Gu, Eva O’Tanyi, William J. Keim, Kenneth W. Rohrbach, Susan Johnghar, Kamelia Behnia, Mary Ann Pelleymounter, Kenneth E. Carlson, William R. Ewing,