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

M. Suehiro, Robert 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 - 1990

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Dopamine D2 Receptors
Papio
Raclopride
Corpus Striatum
Injections
Frontal Lobe
Cerebellum
Carbon
N-methylbenperidol
Brain

ASJC Scopus subject areas

  • Radiological and Ultrasound Technology

Cite this

Suehiro, M., Dannals, R. F., Scheffel, U., Stathis, M., Wilson, A. A., Ravert, H. T., ... 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.

In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol. / Suehiro, M.; Dannals, Robert F; Scheffel, U.; Stathis, M.; Wilson, A. A.; Ravert, H. T.; Villemagne, V. L.; Sanchez-Roa, P. M.; Wagner, H. N.

In: Journal of Nuclear Medicine, Vol. 31, No. 12, 1990, p. 2015-2021.

Research output: Contribution to journalArticle

Suehiro, M, Dannals, RF, Scheffel, U, Stathis, M, Wilson, AA, Ravert, HT, Villemagne, VL, Sanchez-Roa, PM & Wagner, HN 1990, 'In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol', Journal of Nuclear Medicine, vol. 31, no. 12, pp. 2015-2021.
Suehiro M, Dannals RF, Scheffel U, Stathis M, Wilson AA, Ravert HT et al. In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol. Journal of Nuclear Medicine. 1990;31(12):2015-2021.
Suehiro, M. ; Dannals, Robert F ; Scheffel, U. ; Stathis, M. ; Wilson, A. A. ; Ravert, H. T. ; Villemagne, V. L. ; Sanchez-Roa, P. M. ; Wagner, H. N. / In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol. In: Journal of Nuclear Medicine. 1990 ; Vol. 31, No. 12. pp. 2015-2021.
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