99Tcm(CO)3-BPHRGD的制备及正常鼠体内生物分布

⁹⁹Tc^m(CO)₃-BPHRGD的制备及正常鼠体内生物分布

摘要: 制备了⁹⁹Tc^m(CO)₃-BPHRGD，并进行体内外生物学评价。在pH=7、75℃条件下反应30min，⁹⁹Tc^m(CO)₃-BPHRGD的标记率均大于80%，纯化后标记物的放射化学纯度大于98%；体外稳定性实验显示，在37℃时，标记物在生理盐水、胎牛血清及半胱氨酸溶液中具有很好的稳定性；正常小鼠体内生物分布数据显示，⁹⁹Tc^m(CO)₃-BPHRGD在血液中清除较快，主要通过肝肾代谢。

Abstract: ⁹⁹Tc^m(CO)₃-BPHRGD was prepared, and the in vitro and in vivo biological evaluations were completed. The labeling yield of ⁹⁹Tc^m(CO)₃-BPHRGD is more than 80% under optimal conditions(pH=7, reacting at 75℃ for 30 min), and the radiochemical purity is more than 98% after purified. Stability in vitro experiments show that the radiolabeled compound shows good stability in physiological saline, fetal bovine serum, and cysteine solution under 37℃. The biodistribution of ⁹⁹Tc^m(CO)₃-BPHRGD in normal mice shows that the metabolic pathways are mainly though liver and kidney with rapid clearance in blood.