Back to Search
Start Over
In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol.
- Source :
-
Journal of nuclear medicine : official publication, Society of Nuclear Medicine [J Nucl Med] 1990 Dec; Vol. 31 (12), pp. 2015-21. - Publication Year :
- 1990
-
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.
- Subjects :
- Animals
Benperidol chemical synthesis
Benperidol metabolism
Benperidol pharmacokinetics
Brain diagnostic imaging
Brain metabolism
Carbon Radioisotopes
Male
Mice
Papio
Protein Binding
Receptors, Dopamine D2
Tomography, Emission-Computed
Benperidol analogs & derivatives
Receptors, Dopamine metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0161-5505
- Volume :
- 31
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Journal of nuclear medicine : official publication, Society of Nuclear Medicine
- Publication Type :
- Academic Journal
- Accession number :
- 2148346