Imaging benzodiazepine receptors in man with C-11-suriclone and positron emission tomography

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

OSTI ID:6760356

Frost, J J; Dannals, R F; Ravert, H T; Wilson, A A; Links, J M; Trifiletti, R; Snyder, S H; Wagner, Jr, H N

Suriclone is a potent cyclopyrrolone, anti-anxiety drug which binds to the benzodiazepine receptor complex (BZR) with high affinity. Suriclone binds to a site on the BZR distinct from the site where benzodiazepines bind. The K/sub D/ of suriclone at 37oC is 0.03 nM. C-11-suriclone (SUR) was synthesized by reacting C-CH3I with the appropriate amine precursor. SUR (1 ..mu..g/kg) was injected IV into a baboon alone or with 1 mg/kg of Ro-151788, a benzodiazepine antagonist, and serial PET scans of the brain were obtained. High radioactivity concentrations were observed in the cerebral cortex and cerebellum which contain high densities of BZR, intermediate concentrations in thalamus and low concentrations in the striatum. When Ro-151788 was given a uniform distribution of radioactivity was observed; the radioactivity was reduced to ca. 25% of control values in the brain which was contained within the PET slice. SUR (0.2 ..mu..g/kg) was next administered to a human subject. From 30-60 minutes after injection high radioactivity concentrations were observed in the cerebral cortex and cerebellum, intermediate concentrations in the thalamus and a low concentration in the caudate. Radioactivity in the cerebral cortex and cerebellum decreased slowly with time, implying that binding of SUR to a high affinity site had occurred. These results demonstrate utility of SUR for measuring binding to the benzodiazepine receptor complex non-invasively in man.

• Research Organization: The Johns Hopkins Medical Institutions, Baltimore, MD
• OSTI ID: 6760356
• 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

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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BABOONS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BIOCHEMISTRY
BODY
BODY AREAS
BRAIN
CARBON 11
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CEREBELLUM
CEREBRAL CORTEX
CEREBRUM
CHEMISTRY
COMPUTERIZED TOMOGRAPHY
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DIAZO COMPOUNDS
DISTRIBUTION
DOSE-RESPONSE RELATIONSHIPS
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVALUATION
EVEN-ODD NUCLEI
HEAD
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LABELLING
LIGHT NUCLEI
MAMMALS
MAN
MEMBRANE PROTEINS
METABOLISM
MINUTES LIVING RADIOISOTOPES
MONKEYS
NERVOUS SYSTEM
NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
POSITRON COMPUTED TOMOGRAPHY
PRIMATES
PROTEINS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIONUCLIDE KINETICS
RADIOPHARMACEUTICALS
RADIORECEPTOR ASSAY
REACTION KINETICS
RECEPTORS
SCINTISCANNING
THALAMUS
TISSUE DISTRIBUTION
TOMOGRAPHY
TRACER TECHNIQUES
VERTEBRATES