Imaging benzodiazepine receptors in man with C-11-suriclone and positron emission tomography
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-; TRN: 87-010676
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 26:5; Conference: 32. annual meeting of the Society of Nuclear Medicine, Houston, TX, USA, 2 Jun 1985
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
BRAIN
POSITRON COMPUTED TOMOGRAPHY
RADIORECEPTOR ASSAY
SCINTISCANNING
CENTRAL NERVOUS SYSTEM AGENTS
BIOCHEMICAL REACTION KINETICS
DOSE-RESPONSE RELATIONSHIPS
EVALUATION
TISSUE DISTRIBUTION
RADIOPHARMACEUTICALS
BABOONS
BIOCHEMISTRY
CARBON 11
CEREBELLUM
CEREBRAL CORTEX
DIAZO COMPOUNDS
HEAD
LABELLING
MAN
METABOLISM
RADIONUCLIDE KINETICS
RECEPTORS
THALAMUS
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BODY AREAS
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM
CEREBRUM
CHEMISTRY
COMPUTERIZED TOMOGRAPHY
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVEN-ODD NUCLEI
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGHT NUCLEI
MAMMALS
MEMBRANE PROTEINS
MINUTES LIVING RADIOISOTOPES
MONKEYS
NERVOUS SYSTEM
NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PRIMATES
PROTEINS
RADIOISOTOPE SCANNING
RADIOISOTOPES
REACTION KINETICS
TOMOGRAPHY
TRACER TECHNIQUES
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
550501 - Metabolism- Tracer Techniques
550801 - Morphology- Tracer Techniques