New Fluorine-Substituted Analogue of Eticlopride with High Affinity toward Dopamine D2 Receptors

Kiyoko Watanabe, Toshimitsu Fukumura, Shigeki Sasaki, Minoru Maeda, Shuzo Takehara

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Aiming at the development of positron-emitting ligands with specific and high affinity toward dopamine D2 receptors in the central nervous system, we synthesized a new fluorinated eticlopride derivative. A fluorine atom was introduced at the C-4 position of the pyrrolidine ring of eticlopride, a dopamine D2 antagonist of the benzamide series. The in vitro binding affinity of this ligand toward the D2 receptor was found to be as potent as eticlopride, suggesting that the corresponding 18F-labelled compound may be useful as an in vivo radioligand for positron emission tomography.

Original languageEnglish
Pages (from-to)3211-3214
Number of pages4
JournalChemical and Pharmaceutical Bulletin
Volume39
Issue number12
DOIs
Publication statusPublished - Jan 1 1991

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All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Drug Discovery

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