Abstract
Two radioligands, [(11)C] SR149080 and its morpholino analog [(11)C] SR149568, were synthesized by reaction of the respective phenolic precursors with [(11)C] methyl iodide. Both radioligands had appropriate regional brain distribution for cannabinoid receptors in mice with peak target to non-target ratios of 2.2 for [(11)C] SR149080 and 1.6 for [(11)C] SR149568 at 90 and 30 minutes post-injection respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.
Publication types
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Comparative Study
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Evaluation Study
MeSH terms
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Animals
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Brain / diagnostic imaging*
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Brain / metabolism*
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Carbon Radioisotopes / pharmacokinetics*
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Male
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Mice
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Morpholines / chemical synthesis
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Morpholines / pharmacokinetics*
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Piperidines / chemical synthesis
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Piperidines / pharmacokinetics*
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Pyrazoles / chemical synthesis
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Pyrazoles / pharmacokinetics*
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Radionuclide Imaging
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / pharmacokinetics
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Receptors, Cannabinoid
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Receptors, Drug / metabolism*
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Sensitivity and Specificity
Substances
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Carbon Radioisotopes
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Morpholines
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N-(piperidin-1-yl)-5-(4-methoxyphenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
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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 149568