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目的 建立99Tcm 直接标记octreotide的最佳方法 ,评价其受体介导结合特性以及作为肿瘤生长抑素受体显像剂的可能性。方法 采用抗坏血酸钠和连二亚硫酸钠作为还原剂 ,对oct reotide进行标记 ;用大鼠脑皮质细胞膜进行体外受体结合分析 ;进行动物体内分布、药代动力学、毒性实验和临床受体显像。结果 99Tcm octreotide放化纯达 78 5 % ,纯化后为 93 8% ,室温下放置 4h为92 1%。细胞膜体外放射受体结合分析证实99Tcm octreotide与octreotide具有相同的受体介导结合特性。 3例肺癌患者临床受体显像均获得阳性结果。结论 99Tcm 直接法标记octreotide方法可行 ,稳定性好 ;99Tcm octreotide是一种很有希望的肿瘤生长抑素受体显像剂
OBJECTIVE: To establish a 99Tcm optimal method for direct labeling of octreotide to evaluate its receptor-mediated binding properties and its potential as a tumor growth inhibitory receptor imaging agent. Methods Octreotide was labeled with sodium ascorbate and sodium dithionite as reductant. The in vitro receptor binding assay was performed with rat cerebral cortical cell membrane. The in vivo distribution, pharmacokinetics, toxicity and clinical receptor imaging were studied. Results The pure 99Tcm octreotide was 78 5%, 93 8% after purification and 92 1% at room temperature for 4 hours. Cell membrane extracorporeal radioreceptor binding analysis confirmed that 99Tcm octreotide and octreotide have the same receptor-mediated binding properties. Three cases of lung cancer patients with clinical receptor imaging obtained positive results. Conclusion The method of 99Tcm direct labeling octreotide feasible and good stability; 99Tcm octreotide is a promising tumor somatostatin receptor imaging agent