(/sup 18/F)-N-methylspiroperidol: the radioligand of choice for PETT studies of the dopamine receptor in human brain

Journal Article · Tue Jan 01 04:00:00 EST 1985 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(85)90041-4· OSTI ID:6940325

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

N-Methylspiroperidol, the amide N-methyl analogue of the neuroleptic spiroperidol, was radiolabeled with fluorine-18, and its distribution in the baboon brain was studied using positron emission transaxial tomography. Stereospecific binding was demonstrated in the striatum (but not in the cerebellum) by pretreatment with (-)- or (+)-butaclamol. The kinetic distribution was similar to that of (/sup 18/F)spiroperidol, but the absolute striatal uptake (in percent of administered dose) was at least two-fold higher. Analysis of baboon blood at 10 min after injection indicated that less than half of the radioactivity in the plasma was due to unchanged radioligand. Analysis of the metabolic stability of (/sup 18/F)-N-methylspiroperidol in rat brain for 4 hr indicated that, like (/sup 18/F)spiroperidol, it is very stable to metabolic transformation in the rat central nervous system. Striatal uptake and retention in the rat was five-fold higher for (/sup 18/F)-N-methyl-spiroperidol than for (/sup 18/F)spiroperidol. The results suggest that (/sup 18/F)-N-methylspiroperidol is an ideal choice for studies of the dopamine receptor in humans. 25 references, 2 figures, 2 tables.

• Research Organization: Brookhaven National Lab., Upton, NY
• DOE Contract Number: AC02-76CH00016
• OSTI ID: 6940325
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 36; ISSN LIFSA
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMALS
APES
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DOPAMINE
DRUGS
EMISSION COMPUTED TOMOGRAPHY
FLUORINE 18
FLUORINE ISOTOPES
HOURS LIVING RADIOISOTOPES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGANDS
LIGHT NUCLEI
MAMMALS
MAN
MEMBRANE PROTEINS
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
POSITRON COMPUTED TOMOGRAPHY
PRIMATES
PROTEINS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
REACTION KINETICS
RECEPTORS
RODENTS
SYMPATHOMIMETICS
TISSUE DISTRIBUTION
TOMOGRAPHY
TRACER TECHNIQUES
VERTEBRATES