Positron tomography of a radiobrominated analog of SCH 23390: A selective dopamine D1 receptor antagonist
Alterations in the central dopaminergic system have been hypothesized to underlie several neuropsychiatric disorders. Dopamine (DA) receptors in the CNS have been classified into two classes based on whether linkage to the enzyme adenylate cyclase exists, the D1 receptors, or not, D2 receptors. To date, studies on cerebral DA system by positron tomography (PET) have utilized the butyrophenones which are predominantly D2 antagonists. We have prepared Br-75 or Br-76 labelled 8-bromo analog of SCH 23390, (BrSCH), a highly selective antagonist for DA D1 receptors and have measured its distribution in the intact monkey brain by PET and by postmortem section of the mouse brain. An anesthesized 8.5 kg male rhesus monkey was given, i.v., ca. 2 mCi BrSCH on two occasions and scanned with The University of Chicago PETT VI system. Results revealed that the drug localized specifically in the basal ganglia. In a similar experiment in the same monkey given Br-76-bromospiroperidol (BrSP), a predominantly D2 antagonist, high uptake in the basal ganglia was also observed but the time course for specific localization of BrSCH was much faster than that of BrSP. These results provide evidence the D1 receptors, like D2 receptors, are localized in the caudate nucleus (CN) although BrSCH, compared to BrSP, appear to localize more in the posterior aspect of the CN. In conclusion, BrSCH should be a useful imaging agent to study dopamine D1 receptors in the CNS.
- Research Organization:
- Univ. of Chicago, Chicago, IL
- OSTI ID:
- 6719000
- Report Number(s):
- CONF-850611-
- Journal Information:
- J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 26:5; ISSN JNMEA
- Country of Publication:
- United States
- Language:
- English
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62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANESTHESIA
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BASAL METABOLISM
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOLOGICAL LOCALIZATION
BODY
BRAIN
BROMINATION
BROMINE 75
BROMINE 76
BROMINE COMPLEXES
BROMINE ISOTOPES
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
CEREBRUM
CHEMICAL PREPARATION
CHEMICAL REACTIONS
CHEMISTRY
COMPLEXES
COMPUTERIZED TOMOGRAPHY
CYCLASES
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DOPAMINE
DRUGS
EFFICIENCY
ELECTRON CAPTURE RADIOISOTOPES
EMISSION COMPUTED TOMOGRAPHY
ENZYMES
HALOGENATION
HOURS LIVING RADIOISOTOPES
HYDROXY COMPOUNDS
IMMUNOASSAY
IMMUNOLOGY
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
LABELLED COMPOUNDS
LABELLING
LYASES
MACACUS
MAMMALS
MEMBRANE PROTEINS
MENTAL DISORDERS
METABOLISM
MICE
MONKEYS
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-EVEN NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
POSITRON COMPUTED TOMOGRAPHY
PRIMATES
PROTEINS
RADIOASSAY
RADIOCHEMISTRY
RADIOIMMUNOASSAY
RADIOIMMUNOLOGY
RADIOISOTOPES
RADIOPHARMACEUTICALS
RECEPTORS
RODENTS
SYMPATHOLYTICS
SYMPATHOMIMETICS
SYNTHESIS
TISSUE DISTRIBUTION
TOMOGRAPHY
TRACER TECHNIQUES
VERTEBRATES