Abstract
ABSTRACT. [(18)F] SR144385 and [(18)F] SR147963 were synthesized in a multistep reaction in which fluorine-18 was introduced by nucleophilic halogen displacement on a bromo precursor. The fluorine-18-labeled intermediate was deprotected and coupled with the appropriate alkyl amine to give the final products. Both radioligands had appropriate regional brain distribution for cannabinoid receptors with a target to nontarget ratio of 1.7 for [(18)F] SR147963 and 2.5 for [(18)F] SR144385 at 60 and 90 min postinjection, respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.
MeSH terms
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Administration, Inhalation
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Animals
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Brain / diagnostic imaging
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Brain / metabolism*
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Cannabinoids / metabolism*
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Chromatography, High Pressure Liquid
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Fluorine Radioisotopes
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Isotope Labeling
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Ligands
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Male
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Mice
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Morpholines / administration & dosage
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Morpholines / metabolism
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Morpholines / pharmacokinetics*
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Piperidines / administration & dosage
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Piperidines / metabolism
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Piperidines / pharmacokinetics*
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Pyrazoles / administration & dosage
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Pyrazoles / metabolism
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Pyrazoles / pharmacokinetics*
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Radiopharmaceuticals / administration & dosage
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Radiopharmaceuticals / metabolism
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Radiopharmaceuticals / pharmacokinetics*
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Receptors, Cannabinoid
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Receptors, Drug / metabolism*
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Tissue Distribution
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Tomography, Emission-Computed
Substances
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Cannabinoids
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Fluorine Radioisotopes
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Ligands
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Morpholines
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Piperidines
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Pyrazoles
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Radiopharmaceuticals
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Receptors, Cannabinoid
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Receptors, Drug
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SR 144385
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SR 147963