Synthesis and biodistribution of [11C]A-836339, a new potential radioligand for PET imaging of cannabinoid type 2 receptors (CB2).
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ABSTRACT:
SUBMITTER: Horti AG
PROVIDER: S-EPMC2903661 | biostudies-literature | 2010 Jul
REPOSITORIES: biostudies-literature
Publications
Synthesis and biodistribution of [11C]A-836339, a new potential radioligand for PET imaging of cannabinoid type 2 receptors (CB2).
Horti Andrew G AG Gao Yongjun Y Ravert Hayden T HT Finley Paige P Valentine Heather H Wong Dean F DF Endres Christopher J CJ Savonenko Alena V AV Dannals Robert F RF
Bioorganic & medicinal chemistry 20100525 14
Recently, A-836339 [2,2,3,3-tetramethylcyclopropanecarboxylic acid [3-(2-methoxyethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]amide] (1) was reported to be a selective CB2 agonist with high binding affinity. Here we describe the radiosynthesis of [11C]A-836339 ([11C]1) via its desmethyl precursor as a candidate radioligand for imaging CB2 receptors with positron-emission tomography (PET). Whole body and the regional brain distribution of [11C]1 in control CD1 mice demonstrated that this radioligan ...[more]
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