Details

Autor(en) / Beteiligte

• MAEDA, Minoru
• SASAKI, Shigeki
• FUKUMURA, Toshimitsu
• FUKUZAWA, Etsuko
• WATANABE, Kiyoko
• KOJIMA, Masaharu
• TAHARA, Takashi
• MASUDA, Kouji
• ICHIYA, Yuichi

Titel

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

Ist Teil von

• Chemical and Pharmaceutical Bulletin, 1992/07/25, Vol.40(7), pp.1793-1798

Ort / Verlag

Japan: The Pharmaceutical Society of Japan

Erscheinungsjahr

1992

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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 (t1/2=110 min), and their in vivo biodistribution was investigated in rats. N-[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 striata/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 receoptors.