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, T, Sano, H, Yamamoto, Fumihiko, Haradahira, Terushi, Suzuki, Kazutoshi, Suhara, Tetsuya, Sasaki, Shigeki, Maeda, Minoru
Jazyk: angličtina
Rok vydání: 2000
Zdroj: Journal of Labelled Compounds & Radiopharmaceuticals. 43:375-383
ISSN: 0362-4803
Popis: Derivatives of 9,10-ethanobenzo[b]quinolizinium are potent antagonists of 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.
Databáze: OpenAIRE