(+)−3-[125I]碘- mk -801在大鼠脑内与NMDA受体通道复合物的体内结合和放射自显像

Raymond E. Gibson , H.Donald Burns , Holly H. Thorpe , Wai-Si Eng , Richard Ransom , Howard Solomon
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引用次数: 17

摘要

放射性碘化(+)−3-碘- mk -801是n -甲基-d-天冬氨酸(NMDA)受体通道复合物的高亲和力放射性配体。我们已经证明了在大鼠中枢神经系统的体内定位是立体选择性的,并通过联合注射未标记的MK-801阻断。放射自显像显示体内定位,这与体外放射自显像研究一致。这些结果表明,放射性碘化(+)−3-碘- mk -801是一种有效的体外和体内放射自显影研究探针,并表明可以开发出NMDA受体的放射配体,从而提供人体受体分布的体内图像。
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In vivo binding and autoradiographic imaging of (+)−3-[125I]Iodo-MK-801 to the NMDA receptor-channel complex in rat brain

Radioiodinated (+)−3-Iodo-MK-801 is a high affinity radioligand for the N-methyl-d-aspartate (NMDA) receptor-channel complex. We have demonstrated in vivo localization in the CNS of rat which is stereoselective and blocked by coinjection of unlabeled MK-801. Autoradiography indicates localization in vivo which is in concordance with in vitro autoradiographic studies. These results indicate that radioiodinated (+)−3-Iodo-MK-801 is a useful probe for in vitro and in vivo autoradiographic studies and suggest that radioligands for the NMDA receptor may be developed which will provide in vivo images of receptor distribution in man.

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