Radiosynthesis and in vivo evaluation of [¹¹C]4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (methoxy analogue of valdecoxib, [¹¹C]MOV), a COX-2 inhibitor, was conducted in rat and baboon. Synthesis of the reference standard MOV (3), and its desmethyl precursor 2 for radiolabeling were performed using 1,2-diphenylethan-1-one as the starting material in five steps with 15% overall yield. Radiosynthesis of [¹¹C]MOV was accomplished in 40 ± 10% yield and >99% radiochemical purity by reacting the precursor 2 in dimethyl formamide (DMF) with [¹¹C]CH₃I followed by removal of the dimethoxytrityl (DMT) protective group using trifluroacetic acid. PET studies in anesthetized baboon showed very low uptake and homogeneous distribution of [¹¹C]MOV in brain. The radioligand underwent rapid metabolism in baboon plasma. MicroPET studies in male Sprague Dawley rats revealed [¹¹C]MOV binding in lower thorax. The tracer binding in rats was partially blocked in heart and duodenum by the administration of 1 mg/kg oral dose of COX-2 inhibitor valdecoxib.

[ ¹¹ C] 4- [5-（4-甲基苯基）-3-（三氟甲基）-1 H-吡唑-1-基]苯磺酰胺（伐地考昔的甲氧基类似物，[ ¹¹ C] MOV）的放射性合成和体内评价，在大鼠和狒狒中进行了COX-2抑制剂的研究。以1,2-二苯基乙-1-酮为原料，分五个步骤合成参考标准MOV（3）及其用于放射性标记的脱甲基前体2，总产率为15％。[ ¹¹ C] MOV的放射性合成是通过使前体2在二甲基甲酰胺（DMF）中与[ ¹¹ C] CH ₃反应，以40±10％的收率和> 99％的放射化学纯度完成的我随后使用三氟乙酸除去二甲氧基三苯甲基（DMT）保护基。在麻醉的狒狒中进行的PET研究表明，[ ¹¹ C] MOV在大脑中的摄取量非常低且分布均匀。放射性配体在狒狒血浆中快速代谢。在雄性Sprague Dawley大鼠中的MicroPET研究表明，[ ¹¹ C] MOV在下胸腔中具有约束力。通过施用1 mg / kg口服剂量的COX-2抑制剂valdecoxib，大鼠和心脏的示踪剂结合在心脏和十二指肠中被部分阻断。