Synthesis and evaluation of 18F- and 11C-labelled 9,10-ethanobenzo[b]quinolizinium derivatives for imaging of the NMDA receptor at the TCP-binding site

Autor: Ishibashi, Nobuyasu, Kuwamura, Tsuneo, Sano, Hiromi, Yamamoto, Fumihiko, Haradahira, Terushi, Suzuki, Kazutoshi, Suhara, Tetsuya, Sasaki, Shigeki, Maeda, Minoru
Zdroj: Journal of Labelled Compounds and Radiopharmaceuticals; 30 March 2000, Vol. 43 Issue: 4 p375-383, 9p
Abstrakt: 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 [18F]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 [11C]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.
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