Radiobrominated analog of SCH 23390, a selective dopamine D1 antagonist: Synthesis and biodistribution in mouse brain

Conference · Wed May 01 04:00:00 EDT 1985 · J. Nucl. Med.; (United States)

OSTI ID:5938937

De Jesus, O T; Van Moffaert, G J.C.; Glock, D; Dinerstein, R J; Friedman, A M

SCH 23390 (R-(+)-8-chloro-2,3,4, 5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol) is a highly selective dopamine D1 antagonist. The authors have prepared an 8-bromo analog of SCH 23390 (BrSCH) labelled with Br-75 or Br-76 and have studied its distribution in mouse brain. Milligram quantities of BrSCH were synthesized by the reaction of its des-chloro analog with bromide in H/sub 2/O/sub 2/-glacial acetic acid. The product was purified by preparative HPLC and characterized by mass spectrometry, NMR, and a bioassay technique involving the inhibition of DA-induced vasodilation of dog renal artery. Comparison with an authentic sample confirmed that the product obtained was BrSCH. The time course of distribution of this drug in mouse brain was followed and the results showed high uptake in DA receptor-rich striatum. Striatum to cerebellum uptake ratios were observed to be as high as 25 two hours after injection. These results demonstrate that a positron-emitting radiobrominated analog of SCH 23390 would be useful in the imaging of cerebral dopamine D1 receptors.

• Research Organization: Univ. of Chicago, Chicago, IL
• OSTI ID: 5938937
• Report Number(s): CONF-850611-
• Conference Information: Journal Name: J. Nucl. Med.; (United States) Journal Volume: 26:5
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400703 -- Radiochemistry & Nuclear Chemistry-- Radioisotope Production
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
550801 -- Morphology-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
BROMINE 75
BROMINE 76
BROMINE ISOTOPES
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
CHEMICAL PREPARATION
CHEMICAL REACTION YIELD
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DIAGNOSTIC USES
DISTRIBUTION
DOPAMINE
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EMISSION COMPUTED TOMOGRAPHY
HOURS LIVING RADIOISOTOPES
HYDROXY COMPOUNDS
IMMUNOASSAY
IMMUNOLOGY
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LABELLING
MAMMALS
MEMBRANE PROTEINS
MICE
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-EVEN NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
POSITRON COMPUTED TOMOGRAPHY
PROTEINS
RADIOASSAY
RADIOIMMUNOASSAY
RADIOIMMUNOLOGY
RADIOISOTOPES
RADIOPHARMACEUTICALS
RADIORECEPTOR ASSAY
REACTION KINETICS
RECEPTORS
RODENTS
SYMPATHOLYTICS
SYMPATHOMIMETICS
SYNTHESIS
TISSUE DISTRIBUTION
TOMOGRAPHY
TRACER TECHNIQUES
USES
VERTEBRATES
YIELDS