D2-Dopamine receptor specific brain uptake of carbon-11-labeled YM-09151-2

K. Hatano, K. Ishiwata, K. Kawashima, J. Hatazawa, M. Itoh, T. Ido

Research output: Contribution to journalArticlepeer-review

35 Citations (Scopus)

Abstract

The in vivo D2-receptor specific brain uptake of N-[(2RS,3RS)-1-benzyl-2-methyl-3-pyrrolidinyl]-5-chloro-2-methoxy-4-[ 11C]methylaminobenzamide([11C]YM-09151-2), was investigated. In rat brain the high uptake of [11C]YM-09151-2 in striatum was displaced with sulpiride spiroperidol, and YM-09151-2. SCH-23390 and ritanserin, D1-dopamine and S2-serotonin antagonists, showed no effect on the distribution of [11C]YM-09151-2. In the striatum at 60 min, 95% of the radioactivity was detected as [11C]YM-09151-2 by high performance liquid chromatography. On the other hand, 41% of 11C in the plasma at 60 min was observed as metabolites. In vivo autoradiography showed a high uptake of [11C]YM-09151-2 in the striatum and in the nucleus accumbens of rat brain. A high uptake of radioactivity was also found in the canine basal ganglia with positron emission tomography. The uptake was reduced by pretreatment with spiroperidol. The present results demonstrate that [11C]YM-09151-2 is a D2 receptor specific compound and is a potential in vivo tracer for measuring D2 receptors.

Original languageEnglish
Pages (from-to)515-522
Number of pages8
JournalJournal of Nuclear Medicine
Volume30
Issue number4
Publication statusPublished - 1989 Jan 1

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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