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Synthesis and evaluation in vitro and in vivo of a 11C-labeled cyclooxygenase-2 (COX-2) inhibitor
- Source :
-
Bioorganic & Medicinal Chemistry . Aug2008, Vol. 16 Issue 16, p7662-7670. 9p. - Publication Year :
- 2008
-
Abstract
- Abstract: The radiosynthesis and radiopharmacological evaluation of 1-[11C]methoxy-4-(2-(4-(methanesulfonyl)phenyl)cyclopent-1-enyl)-benzene [ 11 C]5 as novel PET radiotracer for imaging of COX-2 expression is described. The radiotracer was prepared via O-methylation reaction with [11C]methyl iodide in 19% decay-corrected radiochemical yield at a specific activity of 20–25GBq/μmol at the end-of-synthesis within 35min. The radiotracer [ 11 C]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 [ 11 C]5 was characterized in male Wistar rats. Compound [ 11 C]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. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 09680896
- Volume :
- 16
- Issue :
- 16
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 33886554
- Full Text :
- https://doi.org/10.1016/j.bmc.2008.07.016