In vivo biodistribution of two ( sup 18 F)-labelled muscarinic cholinergic receptor ligands: 2-( sup 18 F)- and 4-( sup 18 F)-fluorodexetimide
Journal Article
·
· Life Sciences; (USA)
- Johns Hopkins Medical Institutions, Baltimore, MD (USA)
Two ({sup 18}F)-labelled analogues of the potent muscarinic cholinergic receptor (m-AChR) antagonist, dexetimide, were evaluated as potential ligands for imaging m-AChR by positron emission tomography (PET). Intravenous administration of both 2-({sup 18}F)- or 4-({sup 18}F)-fluorodexetimide resulted in high brain uptake of radioactivity in mice. High binding levels were observed in m-AChR rich areas, such as cortex and striatum, with low levels in the receptor-poor cerebellum. Uptake of radioactivity was saturable and could be blocked by pre-administration of dexetimide or atropine. Drugs with different sites of action were ineffective at blocking receptor binding. The results indicate that both radiotracers are promising candidates for use in PET studies.
- OSTI ID:
- 5960933
- Journal Information:
- Life Sciences; (USA), Journal Name: Life Sciences; (USA) Vol. 48:14; ISSN 0024-3205; ISSN LIFSA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DRUGS
EMISSION COMPUTED TOMOGRAPHY
FLUORINE 18
FLUORINE ISOTOPES
HOURS LIVING RADIOISOTOPES
IMAGE PROCESSING
IN VIVO
ISOMERIC TRANSITION ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGANDS
LIGHT NUCLEI
MAMMALS
MEMBRANE PROTEINS
MICE
NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
PARASYMPATHOMIMETICS
POSITRON COMPUTED TOMOGRAPHY
PROCESSING
PROTEINS
RADIOISOTOPES
RADIOPHARMACEUTICALS
REACTION KINETICS
RECEPTORS
RODENTS
TISSUE DISTRIBUTION
TOMOGRAPHY
TRACER TECHNIQUES
VERTEBRATES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DRUGS
EMISSION COMPUTED TOMOGRAPHY
FLUORINE 18
FLUORINE ISOTOPES
HOURS LIVING RADIOISOTOPES
IMAGE PROCESSING
IN VIVO
ISOMERIC TRANSITION ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGANDS
LIGHT NUCLEI
MAMMALS
MEMBRANE PROTEINS
MICE
NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
PARASYMPATHOMIMETICS
POSITRON COMPUTED TOMOGRAPHY
PROCESSING
PROTEINS
RADIOISOTOPES
RADIOPHARMACEUTICALS
REACTION KINETICS
RECEPTORS
RODENTS
TISSUE DISTRIBUTION
TOMOGRAPHY
TRACER TECHNIQUES
VERTEBRATES