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炎症显像是核素影像诊断的重要研究领域,但其中正电子核素标记的药物报道不多。为探索合成一种可特异性在炎症部位浓集、且可鉴别是否为细菌性感染的正电子核素标记的显像剂,我们研究制备了F标记18的Levofloxacin(LVFX)用于炎症显像。标记方法采用经典的Hamacher法(氟离子亲核取代)标记LVFX,放射化学纯大于98%,放射性得率约40%,热原检测为阴性。结果表明标记方法简单迅速,标记物稳定。研究了F-LVFX在正常炎症动物模型内的生物分布以及炎症动物模型的显像。生物分布和显像结果均表明1818F-LVFX在炎症组织内有较高的摄取,炎症组织与正常组织间有显著性差异(P<0.05),该标记物主要通过肾脏和肝脏排泄。研究表明F-LVFX是一种潜在的炎症显像剂。18
Inflammatory imaging is an important research field of radionuclide imaging diagnosis, but positron-nuclide labeled drugs are not widely reported. To explore the synthesis of a positron-neutron-labeled imaging agent that can be specifically concentrated at the site of inflammation and to identify whether it is a bacterial infection, we investigated the preparation of Fv labeled 18 Levofloxacin (LVFX) for inflammatory imaging . Labeling method using the classic Hamacher method (fluoride ion nucleophilic substitution) labeled LVFX, radiochemical pure greater than 98%, radioactive yield of about 40%, pyrogen test was negative. The results show that the labeling method is simple and rapid and the label is stable. Biodistribution of F-LVFX in animal models of normal inflammation and imaging of inflammatory animal models was studied. The results of biodistribution and imaging showed that 1818F-LVFX was upregulated in inflammatory tissues with significant difference (P <0.05) between inflammatory tissues and normal tissues. The markers were mainly excreted in kidney and liver. Studies have shown that F-LVFX is a potential inflammatory imaging agent. 18