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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1565-8. doi: 10.1016/j.bmcl.2010.01.074. Epub 2010 Jan 21.

Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor.

Author information

1
Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.

Abstract

Two novel triaryl ligands 2 and 5 with potent in vitro binding affinities for the cannabinoid subtype-2 (CB2) receptor were labeled with a positron-emitting radioactive nuclide (11)C. Radioligands [(11)C]2, [(11)C]5, and their analogs [(11)C]3 and [(11)C]4 were synthesized by O-[(11)C]methylation of their corresponding phenol precursors with [(11)C]CH(3)I. [(11)C]2-5 had relatively high uptakes (>1.2% injected dose/g tissue) in mouse brains.

PMID:
20137936
DOI:
10.1016/j.bmcl.2010.01.074
[Indexed for MEDLINE]

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