Synthesis and in vivo evaluation of [11C]SEMOTIADIL (cas 116476-13-2), a benzothiazine calcium antagonist
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Add time:08/20/2019 Source:sciencedirect.com
A carbon-11 labeled benzothiazine calcium antagonist, (+)-(R)-2-[5-methoxy-2-[3-[methyl[2-[(3,4-methylenedioxy) phenoxy]ethyl]amino]propoxy]phenyl]-4-methyl-2H-1,4-benzothiazin-3(4H)-one (semotiadil), and its enantiomer were prepared by N-methylation of the corresponding norderivatives with 11CH3I: decay-corrected radiochemical yields of 16 ∼ 27% based on 11CH3I, radiochemical, chemical and optical purity of >99%, sp. act. of 11 ∼ 50 GBq/μmol and preparation time of 35 ∼ 40 min. In mice, saturable and stereo-selective uptake in the hippocampus, striatum and hypothalamus was observed. The potential of the compound to visualize the regional brain calcium channels in vivo by positron emission tomography was indicated; however, no promising sign was found in the myocardium.
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