Synthesis and PET evaluation of (R)??[S??methyl??11C] thionisoxetine, a candidate radioligand for imaging brain norepinephrine transporters

…, A Varrone, B Gulyas, L Farde, C Halldin

文献索引：Schou, Magnus; Pike, Victor W.; Varrone, Andrea; Gulyas, Balazs; Farde, Lars; Halldin, Christer Journal of Labelled Compounds and Radiopharmaceuticals, 2006 , vol. 49, # 11 p. 1007 - 1019

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被引用次数: 16

摘要

Abstract Introduction:(R)-3-(2-(methylthio) phenoxy)-N-methyl-3-phenylpropan-1-amine [(R)– thionisoxetine; 1] is a potent inhibitor of the norepinephrine transporter (NET). We aimed to label 1 with carbon-11 (t 1/2= 20.4 min) for evaluation as a radioligand for imaging NET in living brain with positron emission tomography (PET). Methods: Methyl 3-(2-((R)-3- (methylamino)-1-phenylpropoxy) phenylthio)-propanoate (MPPP) and 1 were each ...