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

Nobuyasu Ishibashi, Tsuneo Kuwamura, Hiromi Sano, Fumihiko Yamamoto, Terushi Haradahira, Kazutoshi Suzuki, Tetsuya Suhara, Shigeki Sasaki, Minoru Maeda

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)375-383
Number of pages9
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume43
Issue number4
DOIs
Publication statusPublished - Mar 30 2000

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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