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目的建立一种由γ计数仪测定放射性肿瘤显像剂锝[99mTc]标记的联肼尼克酰胺-3聚乙二醇-精氨酸-甘氨酸-天冬氨酸环肽二聚体(99mTc-3PRGD2)的方法,并研究肺癌肿瘤模型小鼠注射该显像剂后体内组织分布特点。方法设置4个正常分布组和1个冷肽封闭组(对照组),均经由尾静脉注射该显像剂(8μg/kg)于肺癌肿瘤模型小鼠,正常分布组分别于0.5、1、2和4 h取其组织,对照组在注射放射性药物前0.5 h,腹腔注射0.2 ml 3PRGD2生理盐水溶液(浓度2.5 mg/ml),并于2 h取其组织,肿瘤及其他组织使用γ计数仪检测其放射强度。结果模型小鼠的肿瘤中放射性药物含量很高,脑组织药物透过量极少;肾和膀胱放射性都很高,提示该药物可能主要经肾排泄;对照组小鼠除肾和膀胱外,其他组织的放射性均很低。结论该显像剂具有肿瘤靶向性;冷肽可竞争性地抑制99mTc-3PRGD2与整合素αvβ3受体结合。
OBJECTIVE To establish a method for the determination of radioactive tumor imaging agent technetium [99mTc] labeled hydrazinamide-3 polyethylene glycol-arginine-glycine-aspartic acid cyclic peptide dimer (99mTc-3PRGD2 ), And to study the tissue distribution characteristics of the lung cancer tumor model mice after injecting the imaging agent. Methods Four normal distribution groups and one cold-peptide blocking group (control group) were set up. The imaging agents (8μg / kg) were injected via the tail vein into the lung cancer model mice respectively. Normal distribution groups were 0.5,1,2 (Control group). The control group received intraperitoneal injection of 0.2 ml 3PRGD2 saline solution (2.5 mg / ml) 0.5 h before the injection of radiopharmaceuticals, and the tissues were taken at 2 h. The tumors and other tissues were examined by γ counter Its radiation intensity. Results The tumors in model mice had high levels of radiopharmaceuticals, minimal amounts of drug in brain tissue, high levels of radioactivity in the kidney and bladder, suggesting that the drug may be mainly excreted by the kidneys. In control mice, in addition to the kidneys and bladder, The radioactivity is low. Conclusion The imaging agent has tumor targeting. Cold peptide can competitively inhibit the binding of 99mTc-3PRGD2 to integrin αvβ3 receptor.