Syntheses and biological evaluation of 18F-labeled 3-(1-benzyl-piperidin-4-yl)-1-(1-methyl-1H-indol-3-yl) propan-1-ones for in vivo mapping of acetylcholinesterase
Syntheses and biological evaluation of 18F-labeled 3-(1-benzyl-piperidin-4-yl)-1-(1-methyl-1H-indol-3-yl) propan-1-ones for in vivo mapping of acetylcholinesterase
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DOI：
10.1016/s0969-8051(00)00086-x
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发表时间：
2000-04-01
影响因子：
3.1
通讯作者：
Kim, BT
中科院分区：
文献类型：
--
作者：
Choe, YS;Oh, SJ;Kim, BT
我们合成了新型F-18标记的乙酰胆碱酯酶(AChE)抑制剂，3-[1-(3-和4-[F-18]fluoromethylbenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-ones([F-18]1和[F-18]2)和3-[1-(4-[F-18]fluorobenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-one([F-18]3))，产量高(衰减校正，25%-40%)，并具有高效的特定活动(>；37GBq/亩摩尔)。[F-18]1和[F-18]3在小鼠体内的组织分布研究表明，[F-18]1在脑区具有非特异性结合，并伴有代谢脱氟。这一结果表明，这些放射性配体可能不适合于体内AChE定位，尽管它们在体外具有很强的抗AChE活性。核医学生物27；3：263-267,2000。(C)2000 Elsevier Science Inc.保留所有权利。
We synthesized novel F-18-labeled acetylcholinesterase (AChE) inhibitors, 3-[1-(3- and 4-[F-18]fluoromethylbenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-ones ([F-18]1 and [F-18]2) and 3-[1-(4-[F-18]fluorobenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-one ([F-18]3) in high yields (decay-corrected, 25%-40%) and with high effective specific activities (>37 GBq/mu mol). Tissue distribution studies of the [F-18]1 and the [F-18]3 in mice showed the nonspecific bindings in brain regions, with metabolic defluorination of the [F-18]1. The result suggests that these radioligands may not be suitable agents for in vivo mapping of AChE, despite their potent in vitro anti-AChE activities. NUCL MED BIOL 27;3: 263-267, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.