D2-dopamine receptor specific brain uptake of carbon-11-labeled YM-09151-2

Journal Article · Sat Apr 01 04:00:00 EST 1989 · Journal of Nuclear Medicine; (USA)

OSTI ID:5640672

Hatano, K; Ishiwata, K; Kawashima, K; Hatazawa, J; Itoh, M; Ido, T ^[1]

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1. Tohoku Univ., Sendai (Japan)

The in vivo D2-receptor specific brain uptake of N-((2RS,3RS)-1-benzyl-2- methyl-3-pyrrolidinyl)-5-chloro-2-methoxy-4-({sup 11}C)methylaminobenzamide (({sup 11}C)YM-09151-2), was investigated. In rat brain the high uptake of ({sup 11}C)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 ({sup 11}C)YM-09151-2. In the striatum at 60 min, 95% of the radioactivity was detected as ({sup 11}C)YM-09151-2 by high performance liquid chromatography. On the other hand, 41% of {sup 11}C in the plasma at 60 min was observed as metabolites. In vivo autoradiography showed a high uptake of ({sup 11}C)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 ({sup 11}C)YM-09151-2 is a D2 receptor specific compound and is a potential in vivo tracer for measuring D2 receptors.

• OSTI ID: 5640672
• Journal Information: Journal of Nuclear Medicine; (USA), Journal Name: Journal of Nuclear Medicine; (USA) Vol. 30:4; ISSN 0161-5505; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AUTORADIOGRAPHY
AZAARENES
AZINES
AZOLES
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BRAIN
CARBON 11
CARBON ISOTOPES
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CEREBELLUM
CHROMATOGRAPHY
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DOGS
DOPAMINE
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVEN-ODD NUCLEI
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
LIQUID COLUMN CHROMATOGRAPHY
MAMMALS
MEMBRANE PROTEINS
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PHENOLS
PIPERIDINES
POLYPHENOLS
POSITRON COMPUTED TOMOGRAPHY
PROTEINS
PSYCHOTROPIC DRUGS
PYRIDINES
PYRROLES
RADIOISOTOPES
RADIOPHARMACEUTICALS
RADIOPROTECTIVE SUBSTANCES
RATS
RECEPTORS
RODENTS
SEPARATION PROCESSES
SEROTONIN
SPIPERONE
SYMPATHOMIMETICS
TOMOGRAPHY
TRANQUILIZERS
TRYPTAMINES
UPTAKE
VERTEBRATES