Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 16, Pages 7662-7670Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.07.016
Keywords
positron emission tomography; cyclooxygenase; COX-2 inhibitor; carbon-11; inflammation; cancerogenesis
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The radiosynthesis and radiopharmacological evaluation of 1-[C-11] methoxy-4-(2-(4-(methanesulfonyl)phenyl)cyclopent-1-enyl)-benzene [C-11]5 as novel PET radiotracer for imaging of COX-2 expression is described\. The radiotracer was prepared via O-methylation reaction with [C-11] methyl iodide in 19% decay-corrected radiochemical yield at a specific activity of 20-25 GBq/mu mol at the end-of-synthesis within 35 min. The radiotracer [C-11]5 was evaluated in vitro using various pro-inflammatory and tumor cell lines showing high functional expression of COX-2 at baseline or after induction. In vivo biodistribution of compound [C-11] 5 was characterized in male Wistar rats. Compound [C-11]5 was rapidly metabolized in rat plasma, and more pronounced, in mouse plasma. In vivo kinetics and tumor uptake were demonstrated by dynamic small animal PET studies in a mouse tumor xenograft model. Tumor uptake of radioactivity was clearly visible overtime. However, radioactivity uptake in the tumor could not be blocked by the pre-injection of nonradioactive compound 5. Therefore, it can be concluded that radioactivity uptake in the tumor was not COX-2 mediated. (C) 2008 Elsevier Ltd. All rights reserved.
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