Synthesis and in vivo evaluation of a new fluorine‐18 labeled dopamine D2 radioligand synthesis with benzofuran benzamide skeleton

Futoshi Takao, Shigeki Sasaki, Minoru Maeda, Toshimitsu Fukumura, Takashi Tahara, Kouji Masuda, Yuichi Ichiya

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N‐[(1‐Ethyl‐2‐pyrrolidinyl)methyl]‐5‐(2‐[18F]fluoroethyl)‐2,3‐dihydroben‐zofuran‐7‐carboxamide ([18F]5) was synthesized via nucleophilic substitution with K18F/Kryptofix222 complex in 5.4∼6.8% radiochemical yields with a specific activity of larger than 5.6 TBq/mmol (150 Ci/mmol) at the end of the 110 minutes synthetic period. Its in vivo affinity toward CNS dopamine D2 receptors was investigated using rats in order to evaluate as a radiotracer for the PET (positron emission tomography) study of the dopamine D2 receptors. In biodistribution experiments, [18F]5 exhibited striatal accumulation, although the whole brain radioactivity was cleared rapidly. The striatal/cerebellar radioactivity ratio, which corresponds to the ratio of a brain D2 receptor‐rich to poor region, gradually increased to about 12 at 60 minutes after the injection. The striatal uptake was inhibited with pretreated haloperidol, a dopamine D2 antagonist, indicating that the striatal accumulation was due to the specific binding with D2 receptors. Thus, [18F]5 appears to be a potential in vivo radiotracer for dopamine D2 receptors.

元の言語英語
ページ(範囲)1107-1112
ページ数6
ジャーナルJournal of Labelled Compounds and Radiopharmaceuticals
33
発行部数12
DOI
出版物ステータス出版済み - 12 1993

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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