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[(99m)Tc]MAG(3)-甘露糖基葡聚糖:一种用于前哨淋巴结检测的受体结合放射性药物。

[(99m)Tc]MAG(3)-mannosyl-dextran: a receptor-binding radiopharmaceutical for sentinel node detection.

作者信息

Vera D R, Wallace A M, Hoh C K

机构信息

Department of Radiology, UCSD Cancer Center, University of California, San Diego, School of Medicine, La Jolla, California, USA.

出版信息

Nucl Med Biol. 2001 Jul;28(5):493-8. doi: 10.1016/s0969-8051(01)00218-9.

DOI:10.1016/s0969-8051(01)00218-9
PMID:11516693
Abstract

Technetium-99m-labeled benzoyl-mercaptoacetylglycylglycyl-glycine-mannosyl-dextran ([(99m)Tc]MAG(3)-mannosyl-dextran) is a receptor-binding radiotracer that binds to mannose-binding protein, a receptor expressed by recticuloendothelial tissue. This agent is composed of a 10.5-kilodalton molecule of dextran and multiple units of mannose, and benzoyl-mercaptoacetylglycylglycyl-glycine (BzMAG(3)). The tetraflorophenol-activated ester of BzMAG(3) and the imidate of thiomannose were used to covalently attach BzMAG(3) and mannose to an amino-terminated conjugate of dextran. This yielded a 19-kilodalton macromolecule consisting of 3 BzMAG(3) and 21 mannose units per dextran. Dynamic light scattering was used to measure a mean diameter of 5.5 nanometers for BzMAG(3)-mannosyl-dextran and 0.28 microns for filtered Tc-99m sulfur colloid. A preliminary sentinel node detection study employing right fore and hind footpad injections of [(99m)Tc]MAG(3)-mannosyl-dextran and left fore and hind footpad injections of filtered Tc-99m sulfur colloid demonstrated greater sentinel lymph node uptake by the receptor-binding agent.

摘要

锝-99m标记的苯甲酰-巯基乙酰甘氨酰甘氨酰-甘氨酸-甘露糖基-葡聚糖([(99m)Tc]MAG(3)-甘露糖基-葡聚糖)是一种受体结合放射性示踪剂,它与甘露糖结合蛋白结合,甘露糖结合蛋白是一种由网状内皮组织表达的受体。该试剂由一个10.5千道尔顿的葡聚糖分子、多个甘露糖单元以及苯甲酰-巯基乙酰甘氨酰甘氨酰-甘氨酸(BzMAG(3))组成。BzMAG(3)的四氟苯酚活化酯和硫代甘露糖亚胺用于将BzMAG(3)和甘露糖共价连接到氨基末端的葡聚糖缀合物上。这产生了一个19千道尔顿的大分子,每个葡聚糖由3个BzMAG(3)和21个甘露糖单元组成。动态光散射用于测量BzMAG(3)-甘露糖基-葡聚糖的平均直径为5.5纳米,过滤后的99mTc硫胶体的平均直径为0.28微米。一项初步的前哨淋巴结检测研究,通过右前足和后足注射[(99m)Tc]MAG(3)-甘露糖基-葡聚糖以及左前足和后足注射过滤后的99mTc硫胶体,结果显示受体结合剂在前哨淋巴结中的摄取量更高。

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