INVIVO BIODISTRIBUTION OF 2 [F-18] LABELED MUSCARINIC CHOLINERGIC RECEPTOR LIGANDS - 2-[F-18]-FLUORODEXETIMIDE AND 4-[F-18]-FLUORODEXETIMIDE

被引：19
作者：
WILSON, AA [1 ]
SCHEFFEL, UA [1 ]
DANNALS, RF [1 ]
STATHIS, M [1 ]
RAVERT, HT [1 ]
WAGNER, HN [1 ]
机构：
[1] JOHNS HOPKINS MED INST,DIV RADIAT HLTH SCI,BALTIMORE,MD 21205
来源：
LIFE SCIENCES | 1991年 / 48卷 / 14期
关键词：
D O I：
10.1016/0024-3205(91)90435-E
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
Two [F-18]-labelled analogues of the potent muscarinic cholinergic receptor (m-AChR) antagonist, dexetimide, were evaluated as potential ligands for imaging m-AChR by positron emission tomography (PET). Intravenous administration of both 2-[F-18]- or 4-[F-18]-fluorodexetimide resulted in high brain uptake of radioactivity in mice. High binding levels were observed in m-AChR rich areas, such as cortex and striatum, with low levels in the receptor-poor cerebellum. Uptake of radioactivity was saturable and could be blocked by pre-administration of dexetimide or atropine. Drugs with different sites of action were ineffective at blocking receptor binding. The results indicate that both radiotracers are promising candidates for use in PET studies.
引用
收藏
页码：1385 / 1394
页数：10
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