Positron-Emitting N-[18F]Fluoroalkyl and [18F]Fluoropyrrolidinyl Analogues of Eticlopride as Potential in Vivo Radioligands for Dopamine D2 Receptors

Minoru Maeda, Shigeki Sasaki, Etsuko Fukuzawa, Kiyoko Watanabe, K. Kojima, Toshimitsu Fukumura, Takashi Tahara, Kouji Masuda, Yuichi Ichiya

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12 Citations (Scopus)

Abstract

N-Fluoroalkyl and 4-fluoropyrrolidinyl eticlopride analogues with high affinity toward central nervous system dopamine D2 receptors in vitro were labelled with positron emitting fluorine-18 (fl/2 = 110 min), and their in vivo biodistribution was investigated in rats. 7V-[18F]Fluoro-ethyl and -propyl eticlopride derivatives showed poor in vivo selectivity in the rat brain. On the other hand, 4-[18F]fluoropyrrolidinyl eticlopride exhibited almost constant and relatively high striatal concentration. The striatal/cerebellar radioactivity ratio, which corresponds to the ratio of a brain D2 receptor-rich to poor region, gradually increased to 5.2—6.4, 90 min after the injection. The striatal accumulation was selectively inhibited by pre-injection of haloperidol, a dopamine D2 antagonist, without affecting accumulation in other tissues. Thus, the selective striatal accumulation of 4-[18F]fluoropyrrolidinyl eticlopride in striatal tissue appears to be due to the specific binding to dopamine D2 receptors.

Original languageEnglish
Pages (from-to)1793-1798
Number of pages6
JournalChemical and Pharmaceutical Bulletin
Volume40
Issue number7
DOIs
Publication statusPublished - Jan 1 1992

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Drug Discovery

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