کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371124 981839 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
[11C]Sorafenib: Radiosynthesis and preliminary PET study of brain uptake in P-gp/Bcrp knockout mice
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
[11C]Sorafenib: Radiosynthesis and preliminary PET study of brain uptake in P-gp/Bcrp knockout mice
چکیده انگلیسی

Sorafenib (Nexavar, BAY43-9006, 1) is a second-generation, orally active multikinase inhibitor that is approved for the treatment of some cancers in patients. In this Letter, we developed [11C]1 as a novel positron emission tomography (PET) probe, and evaluated the influence of ABC transporters-mediated efflux on brain uptake using PET with [11C]1 in P-glycoprotein (P-gp)/breast cancer resistance protein (Bcrp) knockout mice versus wild-type mice. [11C]1 was synthesized by the reaction of hydrochloride of aniline 2 with [11C]phosgene ([11C]COCl2) to give isocyanate [11C]6, followed by reaction with another aniline 3. Small-animal PET study with [11C]1 indicated that the radioactivity level (AUC0–60 min, SUV × min) in the brains of P-gp/Bcrp knockout mice was about three times higher than in wild-type mice.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 8, 15 April 2011, Pages 2220–2223
نویسندگان
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