Radiosynthesis of a dopamine receptor-binding radiotracer for positron emission tomography: 3-N-(C-11-methyl)-methyl-spiperone

Conference · Sun Jan 01 04:00:00 EST 1984 · J. Nucl. Med.; (United States)

OSTI ID:6854314

Ravert, H T; Burns, H D; Dannals, R F; Langstrom, B; Duelfer, T; Wilson, A A; Zemyan, S E; Wagner, Jr, H N

Dopamine receptors appear to be involved with abnormalities related to disorders such as Parkinson's disease and schizophrenia. Spiperone is an extremely potent neuroleptic which binds with high affinity to dopamine receptors. Based on in vitro binding studies, the authors selected 3-N-methylspiperone, a derivative of spiperone which has similar binding characteristics, for radiolabeling. C-11 Methyl iodide was prepared from C-11 carbon dioxide and bubbled through a methylene chloride solution of spiperone. Aqueous tetrabutylammonium hydroxide was added with mixing by sonication. The product was isolated by preparative reverse phase high performance liquid chromatography (HPLC) and analyzed for radiochemical purity by analytical C-18 HPLC. Further refinement of the radiochemical synthesis has reduced the time of preparation from an average of 80 minutes to approximately 30 minutes. As many as 5 production runs have been carried out per day. Three are performed routinely due to the shortened synthesis time and the judicious use of remote handling. Automation of the process is now in progress. In 108 consecutive production runs of this radiotracer, the average radiochemical yield has been 35% with an average synthesis time of 36 minutes and the average specific activity of 294 mCi/..mu..mole E.O.S.

• Research Organization: The Johns Hopkins Medical Institutions, Baltimore, MD
• OSTI ID: 6854314
• Report Number(s): CONF-840619-
• Conference Information: Journal Name: J. Nucl. Med.; (United States) Journal Volume: 25:5
• Country of Publication: United States
• Language: English

Related Subjects

37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
400202 -- Isotope Effects
Isotope Exchange
& Isotope Separation
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
550602 -- Medicine-- External Radiation in Diagnostics-- (1980-)
62 RADIOLOGY AND NUCLEAR MEDICINE
AFFINITY
ALKYL RADICALS
AMINES
AROMATICS
AUTOMATION
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BINDING ENERGY
CARBON 11
CARBON COMPOUNDS
CARBON DIOXIDE
CARBON ISOTOPES
CARBON OXIDES
CARDIOTONICS
CARDIOVASCULAR AGENTS
CHALCOGENIDES
CHEMICAL PREPARATION
CHEMISTRY
CHROMATOGRAPHY
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DOPAMINE
DRUGS
EMISSION COMPUTED TOMOGRAPHY
ENERGY
EVEN-ODD NUCLEI
HALOGENATED ALIPHATIC HYDROCARBONS
HYDROXY COMPOUNDS
IN VITRO
IODINATED ALIPHATIC HYDROCARBONS
ISOTOPE APPLICATIONS
ISOTOPES
LABELLED COMPOUNDS
LABELLING
LIGHT NUCLEI
LIQUID COLUMN CHROMATOGRAPHY
MEMBRANE PROTEINS
METHYL IODIDE
METHYL RADICALS
METHYLENE CHLORIDE
MINUTES LIVING RADIOISOTOPES
NEUROREGULATORS
NUCLEI
ORGANIC CHLORINE COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC IODINE COMPOUNDS
OXIDES
OXYGEN COMPOUNDS
PHENOLS
POLYPHENOLS
POSITRON COMPUTED TOMOGRAPHY
PROTEINS
RADICALS
RADIOCHEMISTRY
RADIOISOTOPES
RADIOPHARMACEUTICALS
RECEPTORS
SEPARATION PROCESSES
SYMPATHOMIMETICS
SYNTHESIS
TOMOGRAPHY
TRACER TECHNIQUES