Premium
N ‐methyl‐3‐(1‐hydroxy‐5‐[ 123 I]iodopent‐4‐enyl)‐4‐acetoxypiperidine, a novel candidate of acetylcholinesterase activity imaging agent
Author(s) -
Ueda Takao,
Irie Toshiaki,
Fukushi Kiyoshi,
Ikota Nobuo,
Takatoku Keizo,
Yomoda Isamu,
Nagatsuka ShinIchiro
Publication year - 2000
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/1099-1344(200007)43:8<753::aid-jlcr359>3.0.co;2-#
Subject(s) - chemistry , acetylcholinesterase , radiochemistry , stereochemistry , organic chemistry , enzyme
A novel acetylcholine radioanalog, N ‐methyl‐3‐(1‐hydroxy‐5‐[ 123 I]iodopent‐4‐enyl)‐4‐acetoxypiperidine, was prepared by radioiodination of the corresponding tributylstannyl precursor that was synthesized in eight steps from 4‐piperidone. The tracer has three asymmetric carbons giving eight optical isomers. Two optical isomers were isolated in the precursor synthesis by diastereomeric and enantiomeric separation. In the incubation experiments using rat cerebral cortical homogenate, one optical isomer was hydrolyzed by acetylcholinesterase with high reactivity and selectivity. The tracer is a candidate for mapping cerebral regional acetylcholinesterase activity by single photon emission computed tomography. Copyright © 2000 John Wiley & Sons, Ltd.