کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1878115 | 1042280 | 2009 | 6 صفحه PDF | دانلود رایگان |

Cyclooxygenase (prostaglandin endoperoxide synthase or COX) enzyme represents a particularly attractive target in inflammation processes for the development of both therapeutic agents and imaging agents. This study was designed to develop new radioligands for imaging of inflammation using the biomedical imaging technique positron emission tomography (PET). Carbon-11 labeled celecoxib derivatives, [11C]methyl 2-(4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenylsulfonamidooxy)acetate ([11C]6e), [11C]methyl 2-methyl-2-(4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenylsulfonamidooxy)propanoate ([11C]6f), [11C]methyl 2-(4-(5-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenylsulfonamidooxy)acetate ([11C]6g), and [11C]methyl 2-methyl-2-(4-(5-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenylsulfonamidooxy)propanoate ([11C]6h), were prepared by O-[11C]methylation of their corresponding precursors using [11C]CH3OTf under basic condition and isolated by a simplified solid-phase extraction (SPE) method in 50–60% radiochemical yields based on [11C]CO2 and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 15–20 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 111–185 GBq/μmol.
Journal: Applied Radiation and Isotopes - Volume 67, Issue 11, November 2009, Pages 2019–2024