(3-N-(/sup 11/C)methyl)spiperone, a ligand binding to dopamine receptors: radiochemical synthesis and biodistribution studies in mice

Journal Article · Thu Nov 01 04:00:00 EST 1984 · J. Nucl. Med.; (United States)

OSTI ID:6215974

Burns, H D; Dannals, R F; Langstroem, B; Ravert, H T; Zemyan, S E; Duelfer, T; Wong, D F; Frost, J J; Kuhar, M J; Wagner, H N

Carbon-11-labeled 3-N-methylspiperone, a positron-emitting dopamine-receptor antagonist with potential for use in positron emission tomography studies of human neurotransmitter receptors, was synthesized from /sup 11/CO/sub 2/ in 40 minutes, with a radiochemical yield of approx. 20-40%. The specific activity of the (3-N-(/sup 11/C)methyl)-spiperone was determined by ultraviolet spectroscopy to be approximately 270 mCi/..mu..mol at the end of synthesis. In in vitro binding experiments, the K/sub i/ for 3-N-methylspiperone was found to be approximately 250 pM (against H-3 spiperone). The brain-to-blood ratios in normal ICR mice were 2.8 or greater at the times studied, and the striatum-to-cerebellum ratio at 60 minutes at injection was 20:1.

• Research Organization: Johns Hopkins Medical Institutions, Baltimore, MD
• OSTI ID: 6215974
• Journal Information: J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:11; 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
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BODY
BODY FLUIDS
BRAIN
CARBON 11
CARBON COMPOUNDS
CARBON DIOXIDE
CARBON ISOTOPES
CARBON OXIDES
CARDIOTONICS
CARDIOVASCULAR AGENTS
CARDIOVASCULAR SYSTEM
CENTRAL NERVOUS SYSTEM
CHALCOGENIDES
CHEMICAL PREPARATION
CHEMICAL REACTION YIELD
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DIGESTIVE SYSTEM
DISTRIBUTION
DOPAMINE
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVEN-ODD NUCLEI
GLANDS
HEART
HYDROXY COMPOUNDS
ISOTOPES
KIDNEYS
LABELLED COMPOUNDS
LIGANDS
LIGHT NUCLEI
LIVER
LUNGS
MAMMALS
MATERIALS
MICE
MINUTES LIVING RADIOISOTOPES
MUSCLES
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ORGANIC COMPOUNDS
ORGANS
OXIDES
OXYGEN COMPOUNDS
PHENOLS
POLYPHENOLS
POSITRON COMPUTED TOMOGRAPHY
RADIOISOTOPES
RADIOPHARMACEUTICALS
RECEPTORS
RESPIRATORY SYSTEM
RODENTS
SYMPATHOMIMETICS
SYNTHESIS
TISSUE DISTRIBUTION
TOMOGRAPHY
VERTEBRATES
YIELDS