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Synthesis and evaluation of 18 F‐ and 11 C‐labelled 9,10‐ethanobenzo[ b ]quinolizinium derivatives for imaging of the NMDA receptor at the TCP‐binding site
Author(s) -
Ishibashi Nobuyasu,
Kuwamura Tsuneo,
Sano Hiromi,
Yamamoto Fumihiko,
Haradahira Terushi,
Suzuki Kazutoshi,
Suhara Tetsuya,
Sasaki Shigeki,
Maeda Minoru
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/(sici)1099-1344(20000330)43:4<375::aid-jlcr324>3.0.co;2-q
Subject(s) - chemistry , nmda receptor , biodistribution , methylation , fluoride , stereochemistry , fluorine , receptor , organic chemistry , biochemistry , in vitro , inorganic chemistry , gene
Derivatives of 9,10‐ethanobenzo[ b ]quinolizinium are potent antagonists for the TCP‐site of the NMDA receptor. Two fluoroethyl‐substituted analogues were labelled with fluorine‐18 by displacement of the tosylate with [ 18 F]fluoride, followed by a Diels‐Alder reaction. A methoxy‐substituted analogue labelled with carbon‐11 was obtained by O‐methylation of the corresponding hydroxy precursor with [ 11 C]iodomethane. In biodistribution studies in mice with these three radioligands, it was found that they have little ability to penetrate the blood‐–brain barrier. Copyright © 2000 John Wiley & Sons, Ltd.