Compounds derived from celecoxib and valdecoxib, and methods of use thereof, are disclosed. The compounds are useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The compounds contain a radioactive agent which permits imaging. The compounds concentrate at sites of increased cyclooxygenase expression, such as areas of increased COX-2 expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections, assessing efficacy of diagnosis and treatment of rheumatoid arthritis, and assessing the need for treatment with opioid drugs.
本文披露了从Celecoxib和Valdecoxib衍生的化合物及其使用方法。这些化合物可用于识别和定位导致患者疼痛感的病理和/或炎症部位;用于识别原发、继发、良性或恶性肿瘤的部位;以及用于诊断感染或确认或排除疑似感染。这些化合物含有放射性物质,可用于成像。这些化合物会聚集在环氧合酶表达增加的部位,如COX-2表达增加的区域,从而揭示了与疼痛和炎症相关的
前列腺素产生增加的部位,并与肿瘤存在和/或位置相关。识别COX表达增加的区域还可用于筛查感染,评估类风湿关节炎的诊断和治疗的疗效,以及评估是否需要使用阿片类药物治疗。