Synthesis and evaluation of new 18F-labelled thienylcyclohexylpiperidine (TCP) analogues as radioligands for the NMDA receptor-channel complex

Y. Shibayama, S. Sasaki, U. Tomita, T. Nishikawa, M. Maeda

研究成果: ジャーナルへの寄稿学術誌査読

16 被引用数 (Scopus)

抄録

We have synthesized new fluorine-18 labelled derivatives of thienylcyclohexylpiperidine (TCP), a non-competitive antagonist of NMDA receptor, which binds to the phencyclidine (PCP) binding site located within the receptor-associated ion channel. The mesylate precursors for (1S*,2R*)-2-(hydroxymethyl)- and (1S*,2R*)-2-(methoxymethyoxymethyl)-1-(N-piperidyl)-1-[2-(2'-[18F] fluoroethyl)thiophenyl]cyclohexane, [18F]4 and [18F]19, respectively, were prepared from 2-hydroxycyclo-hexanone. Radiochemical syntheses were done by displacement of the mesylates by [18F]fluoride ion with no-carrier-added [K/2.2.2]+18F in 4-4.5% radiochemical yields with specific activity of >31 GBq/mol. In the biodistribution studies with [18F]4 and [18F]19, no selective accumulation of radioactivity was observed. Low affinities of these ligands to the NMDA receptor were also shown in in vitro binding experiments.

本文言語英語
ページ(範囲)77-86
ページ数10
ジャーナルJournal of Labelled Compounds and Radiopharmaceuticals
38
1
DOI
出版ステータス出版済み - 1996

!!!All Science Journal Classification (ASJC) codes

  • 分析化学
  • 生化学
  • 放射線学、核医学およびイメージング
  • 創薬
  • 分光学
  • 有機化学

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