| ~(99)Tc~m-MAG_3-K237的制备及其在健康动物体内的药代动力学和分布研究 |
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| 引用本文： | 杨明福,刘广元,李前伟.~(99)Tc~m-MAG_3-K237的制备及其在健康动物体内的药代动力学和分布研究[J].第三军医大学学报,2010,32(5). |
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| 作者姓名： | 杨明福 刘广元 李前伟 |
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| 作者单位： | 第三军医大学西南医院核医学科,重庆,400038 |
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| 摘 要： | 目的探讨99Tcm标记血管内皮生长因子受体2(vascular endothelial growth factor receptor-2,VEGFR-2,KDR)小分子拮抗肽K237的方法,研究标记物在健康动物体内的药代动力学特性及体内分布特点。方法化学方法合成制备MAG3-K237,并用99Tcm标记;鉴定标记物的理化性质;测定标记物经新西兰大白兔静脉注射后不同时相血液放射性浓度,得出最佳房室模型与药代动力学参数;分别测定经尾静脉注射7.4MBq标记物后的昆明小鼠各器官质量和放射性计数,经参考源校正后计算各脏器每克组织百分注射剂量率(%ID/g);经耳缘静脉注射37MBq标记物,在SPECT下观察其在兔体内的动态分布。结果99Tcm-MAG3-K237的放化纯度为(97.98±0.76)%,比活度为(3.54±0.03)TBq/mmol;室温(25℃)下保存8h后放化纯度为(96.15±0.37)%;半胱氨酸置换率为0.2%～0.37%;不与血清蛋白结合;兔体内动力学过程符合权重为1/c2的三室模型,快分布相半衰期(t1/2α)、慢分布相半衰期(t1/2β)及消除相半衰期(t1/2γ)分别为(4.00±3....
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| 关 键 词： | 血管生成抑制剂 血管内皮生长因子受体2 药代动力学 放射性核素显像 K237 组织分布 兔 小鼠 |
Preparation of ~(99)Tc~m-MAG_3-K237 and its pharmacokinetics and distribution in health animals |
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| Yang Mingfu,Liu Guangyuan,Li Qianwei.Preparation of ~(99)Tc~m-MAG_3-K237 and its pharmacokinetics and distribution in health animals[J].Acta Academiae Medicinae Militaris Tertiae,2010,32(5). |
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| Authors: | Yang Mingfu Liu Guangyuan Li Qianwei |
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| Institution: | Department of Nuclear Medicine;Southwest Hospital;Third Military Medical University;Chongqing;400038;China |
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| Abstract: | Objective To explore how to label small molecule inhibitor K237(HTMYYHHYQHHL) of vascular endothelial growth factor receptor-2(VEGFR-2,KDR) with technetium 99m and to study pharmacokinetic characteristics and body distribution of the labeled peptide in healthy animals.Methods MAG3K237 was prepared through chemosynthesis,and then labeled it with 99 Tcm.Then its stability and physicochemical properties were determined by paper chromatography.The best compartment model and its pharmacokinetic parameters were o... |
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| Keywords: | angiogenesis inhibitors vascular endothelial growth factor receptor-2 pharmacokinetics radionuclide imaging K237 tissue distribution rabbits mice |
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