In vivo study of drug interaction with brain benzodiazepine receptor
Conference
·
· J. Nucl. Med.; (United States)
OSTI ID:6700943
The possibility of direct estimation of in vivo Bz receptor occupancy in brain was evaluated using C-11, or H-3-flumazepil (Ro15-1788). In animal experiments, 1 ..mu..Ci of H-3-Ro15-1788 was injected at 0.5 or 20 hr after i.v. injection of various dosage of clonazepam. Then radioactivity in cerebral cortex, cerebellum and blood at 5 min. after injection of the tracer was compared. Competitive inhibition of in vivo binding was clearly observed when clonazepam was pretreated at 0.5 hr before injection of the tracer. On the other hand, brain radioactivity was increased when clonazepam was administered at 20 hr before injection of the tracer. This increase in binding of H-3-Ro15-1788 might be caused by rebound of Bz receptor function by treatment with Bz agonist, and this rebound may have an important role in physiological function. Clinical investigation concerning drug interaction with brain Bz receptor was performed in normal volunteer and patients with neurological disorders. The distribution of C-11-Ro15-1788 in the brain of patients chronically treated with clonazepam were significantly heterogeneous. However, cerebral blood flow estimated with N-13 NH3 of these patients were normal.
- Research Organization:
- Div. of Clinical Research, National Institute of Radiological Sciences, Chiba
- OSTI ID:
- 6700943
- 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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Related Subjects
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL LOCALIZATION
BIOLOGICAL MATERIALS
BLOOD
BLOOD FLOW
BODY
BODY FLUIDS
BRAIN
CARBON 11
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CEREBELLUM
CEREBRAL CORTEX
CEREBRUM
CHEMICAL BONDS
DIAGNOSIS
DISEASES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EVEN-ODD NUCLEI
IN VIVO
INHIBITION
INJECTION
INTAKE
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGHT NUCLEI
MATERIALS
MEMBRANE PROTEINS
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NERVOUS SYSTEM DISEASES
NITROGEN 13
NITROGEN ISOTOPES
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PATIENTS
PROTEINS
PSYCHOTROPIC DRUGS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RADIORECEPTOR ASSAY
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
TRANQUILIZERS
62 RADIOLOGY AND NUCLEAR MEDICINE
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL LOCALIZATION
BIOLOGICAL MATERIALS
BLOOD
BLOOD FLOW
BODY
BODY FLUIDS
BRAIN
CARBON 11
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CEREBELLUM
CEREBRAL CORTEX
CEREBRUM
CHEMICAL BONDS
DIAGNOSIS
DISEASES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EVEN-ODD NUCLEI
IN VIVO
INHIBITION
INJECTION
INTAKE
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGHT NUCLEI
MATERIALS
MEMBRANE PROTEINS
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NERVOUS SYSTEM DISEASES
NITROGEN 13
NITROGEN ISOTOPES
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PATIENTS
PROTEINS
PSYCHOTROPIC DRUGS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RADIORECEPTOR ASSAY
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
TRANQUILIZERS