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本工作以舒必利 (Sulpiride)为分子模型 ,在芳环的 5位上引入巯基 (替代磺酰胺基 )合成了 (S) -(- ) - 5-巯基 - N- [(1 -乙基 - 2 -吡咯烷基 )甲基 ] - 2 -甲氧基苯甲酰胺 [简写为 MBZM ]左旋异构体。通过“3+1”(二元混合配体络合 )方案 ,合成了一种新的 D2受体显像剂 99Tcm - MBZM。其在大鼠体内的生物分布实验结果显示 ,99Tcm- MBZM在血液中的清除较快 ,30 min后降到 0 .444% ID/ g;在肝和肾脏中的放射性则持续较高 ,30 min后仍分别达 2 .1 4 8和 2 .1 84% ID/ g;在脑中的摄取量偏低 ,2 min时仅为 0 .1 4 5 % ID/ g。因此 99Tcm - MBZM不能作为脑受体显像剂。
(S) - (-) - 5-mercapto-N- [(1-ethyl-2-pyrazol-2-yl) sulfonyl chloride was synthesized using sulpiride as the molecular model - pyrrolidinyl) methyl] -2-methoxybenzamide [abbreviated as MBZM] levorotatory isomer. A novel D2 receptor imaging agent 99Tcm - MBZM was synthesized by “3 + 1” (binary mixed ligand complexation) protocol. The results of its biodistribution in rat showed that 99Tcm-MBZM was cleared rapidly in the blood and dropped to 0.444% ID / g after 30 min. The radioactivity of 99Tcm-MBZM was consistently high in the liver and kidney at 30 min Still up to 2.148 and 2 .1 84% ID / g, respectively; their uptake in the brain was low, only 0.145% ID / g at 2 min. Therefore, 99Tcm - MBZM can not be used as brain receptor imaging agent.