@article{oai:repo.qst.go.jp:00046041, author = {Asakawa, Chiharu and Ogawa, Masanao and Kumata, Katsushi and Fujinaga, Masayuki and Kato, Koichi and Yamasaki, Tomoteru and Yui, Joji and Kawamura, Kazunori and Hatori, Akiko and Fukumura, Toshimitsu and Zhang, Ming-Rong and 浅川 千春 and 小川 政直 and 熊田 勝志 and 藤永 雅之 and 加藤 孝一 and 山崎 友照 and 由井 譲二 and 河村 和紀 and 羽鳥 晶子 and 福村 利光 and 張 明栄}, issue = {8}, journal = {Bioorganic & Medicinal Chemistry Letters}, month = {Apr}, note = {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 x min) in the brains of P-gp/Bcrp knockout mice was about three times higher than in wild-type mice.}, pages = {2220--2223}, title = {[11C]Sorafenib: Radiosynthesis and preliminary PET study of brain uptake in P-gp/Bcrp knockout mice}, volume = {21}, year = {2011} }