DESIGN AND EVALUATION OF RADIOACTIVE ACETYLCHOLINE ANALOGS FOR MAPPING BRAIN ACETYLCHOLINESTERASE (ACHE) IN-VIVO

被引：105

作者：

IRIE, T

FUKUSHI, K

AKIMOTO, Y

TAMAGAMI, H

NOZAKI, T

机构：

[1] TOHO UNIV, FAC PHARM, CHIBA 274, JAPAN

[2] KITASATO UNIV, FAC HYG SCI, KANAGAWA 228, JAPAN

来源：

NUCLEAR MEDICINE AND BIOLOGY | 1994年 / 21卷 / 06期

关键词：

D O I：

10.1016/0969-8051(94)90159-7

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

For mapping brain acetylcholinesterase (AchE) in vivo, seven radioactive acetylcholine analogs, N-[C-14]methylpiperidyl-3- and 4-acetates, propionates, isobutyrates, and 3-butyrate were newly synthesized and evaluated in mice. The esters readily entered the brain and were hydrolyzed into the hydrophilic metabolite, which was trapped. In brain homogenates, the esters showed a wide range of enzymatic reactivity (about 40-fold), and high specificity for AchE (more than 82%) except the butyrate. Intra-brain distribution of the esters reflected a pattern of AchE activity.

引用

页码：801 / 808

页数：8

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