Substituted benzamides as ligands for visualization of dopamine receptor binding in the human brain by positron emission tomography
Two substituted benzamides, FLB 524 and raclopride, were labeled with C and examined for their possible use as ligands for positron emission tomography (PET) scan studies on dopamine-2 (D-2) receptors in the brains of monkeys and healthy human subjects. Both ligands allowed the in vivo visualization of D-2 receptor binding in the corpus striatum caudate nucleus/putamen complex in PET-scan images. ( C)Raclopride showed a high ratio of specific striatal to nonspecific cerebellar binding, and the kinetics of binding of this ligand made it optimal for PET studies. The in vivo binding of ( C)raclopride in the striatum of cynomolgus monkeys was markedly reduced by displacement with haloperidol. In healthy human subjects, ( C)raclopride binding in the caudate nucleus/putamen was 4- to 5-fold greater than nonspecific binding in the cerebellum. In comparison with previously available ligands for PET-scan studies on central dopamine receptors in man, ( C)raclopride appears to be advantageous with regard to (i) specificity of binding to D-2 receptors, (ii) the high ratio between binding in dopamine-rich (caudate, putamen) and dopamine-poor (cerebellum) human brain regions, and (iii) rapid association and reversibility of specific binding.
- Research Organization:
- Karolinska Institute, Stockholm, Sweden
- OSTI ID:
- 6289618
- Journal Information:
- Proc. Natl. Acad. Sci. U.S.A.; (United States), Vol. 82:11
- Country of Publication:
- United States
- Language:
- English
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63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
BRAIN
POSITRON COMPUTED TOMOGRAPHY
RADIONUCLIDE KINETICS
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
AMIDES
CARBON 11
CARBON DIOXIDE
DOPAMINE
MAN
MONKEYS
RECEPTORS
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
CARBON COMPOUNDS
CARBON ISOTOPES
CARBON OXIDES
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
CHALCOGENIDES
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVEN-ODD NUCLEI
HYDROXY COMPOUNDS
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
MAMMALS
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
OXIDES
OXYGEN COMPOUNDS
PHENOLS
POLYPHENOLS
PRIMATES
RADIOISOTOPES
SYMPATHOMIMETICS
SYNTHESIS
TOMOGRAPHY
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
400702 - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials
560171 - Radiation Effects- Nuclide Kinetics & Toxicology- Man- (-1987)
560172 - Radiation Effects- Nuclide Kinetics & Toxicology- Animals- (-1987)