D2-dopamine receptor specific brain uptake of carbon-11-labeled YM-09151-2.
J Nucl Med
; 30(4): 515-22, 1989 Apr.
Article
em En
| MEDLINE
| ID: mdl-2567779
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.
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Base de dados:
MEDLINE
Assunto principal:
Antipsicóticos
/
Benzamidas
/
Encéfalo
/
Receptores Dopaminérgicos
Limite:
Animals
Idioma:
En
Ano de publicação:
1989
Tipo de documento:
Article