Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Radiosynthesis and Biodistribution in Mice of a 18F-Labeled Analog of O-1302 for Use in Cerebral CB1 Cannabinoid Receptor Imaging
Yumiko NojiriKiichi IshiwataQinggeletuShintaro TobiishiToru SasadaFumihiko YamamotoTakahiro MukaiMinoru Maeda
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2008 Volume 31 Issue 6 Pages 1274-1278


The suitability of an 18F-labeled form of N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-5-{4′-(5-fluoropentyl)phenyl}-4-methyl-1H-pyrazole-3-carboxamide (1), a CB1 cannabinoid ligand with high binding affinity (Ki=0.91 nM) and moderate lipophilicity (log P7.4=2.9), as a radiotracer for positron emission tomography imaging was evaluated in mice. Ligand 1 was labeled with 18F (T1/2=109.7 min) by treatment of the corresponding tosyl derivative with [18F]fluoride ion in acetonitrile. Tissue distribution studies of the 18F-labeled form ([18F]1) in mice demonstrated low brain uptake with minimal specific binding in brain regions. Cyclosporin A ( a modulator of P-glycoprotein) treatment significantly increased both the brain uptake and the brain-to-blood ratio of [18F]1, indicating the possibility that P-glycoprotein regulates the ability of [18F]1 to cross the blood brain barrier. Radioligand [18F]1 does not have the required properties for imaging the cerebral cannabinoid CB1 receptor in vivo.

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© 2008 The Pharmaceutical Society of Japan
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