In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol

M. Suehiro, R. F. Dannals, U. Scheffel, M. Stathis, A. A. Wilson, H. T. Ravert, V. L. Villemagne, P. M. Sanchez-Roa, H. N. Wagner

Research output: Contribution to journalArticle

Abstract

A new dopamine D2 receptor radiotracer, N-11C-methyl-benperidol (11C-NMB), was prepared and its in vivo biologic behavior in mice and a baboon was studied. Carbon-11-NMB was determined to bind to specific sites characterized as dopamine D2 receptors. The binding was saturable, reversible, and stereospecific. Kinetic studies in the dopamine D2 receptor-rich striatum showed that 11C-NMB was retained five times longer than in receptor-devoid regions, resulting in a high maximum striatal-to-cerebellar ratio of 11:1 at 60 min after injection. From frontal cortex and cortex, on the other hand, the tracer washed out as rapidly as it did from cerebellum, resulting in tissue-to-cerebellar ratios close to one in these regions at any time after injection. Blocking studies confirmed the specificity and selectivity of the 11C-NMB binding to the dopamine D2 receptor. A PET study with 11C-NMB of the baboon brain revealed highly selective labeling of dopamine D2 receptor sites which was blocked by preinjection of raclopride.

Original languageEnglish (US)
Pages (from-to)2015-2021
Number of pages7
JournalJournal of Nuclear Medicine
Volume31
Issue number12
StatePublished - Dec 1 1990

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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    Suehiro, M., Dannals, R. F., Scheffel, U., Stathis, M., Wilson, A. A., Ravert, H. T., Villemagne, V. L., Sanchez-Roa, P. M., & Wagner, H. N. (1990). In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol. Journal of Nuclear Medicine, 31(12), 2015-2021.