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

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

研究成果: Contribution to journalArticle査読

4 被引用数 (Scopus)

抄録

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.

本文言語英語
ページ(範囲)3211-3214
ページ数4
ジャーナルChemical and Pharmaceutical Bulletin
39
12
DOI
出版ステータス出版済み - 1991

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Drug Discovery

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