No-carrier-added fluorine-18-labeled N-methylspiroperidol: synthesis and biodistribution in mice

Journal Article · Sat Feb 01 00:00:00 EST 1986 · J. Nucl. Med.; (United States)

OSTI ID:5232886

Shiue, C Y; Fowler, J S; Wolf, A P; McPherson, D W; Arnett, C D; Zecca, L

No-carrier-added fluorine-18- (18F) labeled N-methylspiroperidol (4) was synthesized from four different substrates: p-nitrobenzonitrile (1), cyclopropyl p-nitrophenyl ketone (2A), p-cyclopropanoyl-N,N,N-trimethylanilinium iodide (2B) and p-cyclopropanoyl-N,N,N-trimethylanilinium perchlorate (2C) using the nucleophilic aromatic substitution reaction. Radiochemical yield, synthesis time, experimental simplicity, and specific activity were compared. In addition, factors which influence the yield of the nucleophilic aromatic substitution were studied. Based on these studies, the synthesis of 4 from 2A maximizes product specific activity and experimental simplicity and provides 4 in 10-15% radiochemical yield (based on (18F-) with a mass of less than 2 nmol and a specific activity of greater than 10 Ci/mumol (EOB)). The synthesis of 4 from 8-(4-(4-nitrophenyl)-4-oxobutyl)-3-methyl-1-phenyl-1,3,8-triazaspiro+ ++ (4.5)decan-4-one (5) and Cs(18F) using the nucleophilic aromatic substitution reaction gave unacceptably low and erratic yields. The biodistribution of 4 in mice showed a maximum brain uptake of 1.1% of the administered dose at 5 min and declined to approximately 0.6% at 120 min.

• Research Organization: Brookhaven National Lab., Upton, NY
• OSTI ID: 5232886
• Journal Information: J. Nucl. Med.; (United States), Vol. 2
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
FLUORINE 18
TISSUE DISTRIBUTION
LABELLED COMPOUNDS
CHEMICAL PREPARATION
BRAIN
LABELLING
MICE
RADIOCHEMISTRY
UPTAKE
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
CENTRAL NERVOUS SYSTEM
CHEMISTRY
DISTRIBUTION
FLUORINE ISOTOPES
HOURS LIVING RADIOISOTOPES
ISOTOPES
LIGHT NUCLEI
MAMMALS
NERVOUS SYSTEM
NUCLEI
ODD-ODD NUCLEI
ORGANS
RADIOISOTOPES
RODENTS
SYNTHESIS
VERTEBRATES
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