SYNTHESIS AND IN-VIVO EVALUATION OF [C-11] SEMOTIADIL, A BENZOTHIAZINE CALCIUM-ANTAGONIST

被引：20

作者：

ISHIWATA, K ^{[1
]}

SEKI, H ^{[1
]}

ISHII, K ^{[1
]}

ISHII, S ^{[1
]}

NOZAKI, T ^{[1
]}

SENDA, M ^{[1
]}

机构：

[1] KITASATO UNIV,FAC HYG SCI,SAGAMIHARA,KANAGAWA 228,JAPAN

来源：

APPLIED RADIATION AND ISOTOPES | 1994年 / 45卷 / 04期

关键词：

D O I：

10.1016/0969-8043(94)90108-2

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

A carbon-11 labeled benzothiazine calcium antagonist, (+)-(R)-2-[5-methoxy-2-]3-[methyl[2-](3,4-methylenedioxy)phenoxylethyl]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 (CH3I)-C-11: decay-corrected radiochemical yields of 16 - 27% based on (CH3I)-C-11, radiochemical, chemical and optical purity of >99%, sp. act. of 11 - 50GBq/mumol 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.

引用

页码：439 / 443

页数：5