In Vivo Labeling of the Dopamine D2 Receptor with N-11C-Methyl-Benperidol

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 stereo...

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Published inThe Journal of nuclear medicine (1978) Vol. 31; no. 12; pp. 2015 - 2021
Main Authors Suehiro, Makiko, Dannals, Robert F, Scheffel, Ursula, Stathis, Marigo, Wilson, Alan A, Ravert, Hayden T, Villemagne, Victor L, Sanchez-Roa, Patricia M, Wagner, Henry N., Jr
Format Journal Article
LanguageEnglish
Published Reston, VA Soc Nuclear Med 01.12.1990
Society of Nuclear Medicine
Subjects
Animals
Benperidol - analogs & derivatives
Benperidol - chemical synthesis
Benperidol - metabolism
Benperidol - pharmacokinetics
Biological and medical sciences
Brain - diagnostic imaging
Brain - metabolism
Carbon Radioisotopes
Investigative techniques, diagnostic techniques (general aspects)
Male
Medical sciences
Mice
Papio
Protein Binding
Receptors, Dopamine - metabolism
Receptors, Dopamine D2
Tomography, Emission-Computed
In vivo
D2 Dopamine receptor
Radiolabelling
Nitrogen
Radiopharmaceuticals
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Summary: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.
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ISSN:0161-5505
1535-5667