【摘要】 以fac-[188Re(CO)3(H2O)3]+为前体标记了含RGD的环状多肽H-c(RGDyK)(Pc1):75℃下反应30 min即可得到标记率和放化产率大于90%的目标产物188Re(CO)3-Pc1。此标记物在小牛血清及磷酸缓冲液(pH=7.4)中稳定性良好,Pc1对U87 MG细胞有良好的亲和力,半抑制常数(IC50)为84.9 nmol/L。生物分布数据显示,188Re-Pc1在血液内清除较快,且通过肝胆和肾代谢排出体外;在肿瘤内有一定的摄取。更多还原

【Abstract】 A cyclic RGD containing peptide H-c(RGDyK)(Pc1) was labeled with 188Re using fac-[188Re(CO)3(H2O)3] as the precursor.The radiolabeling yield and radiochemical purity were more than 90% with in 30 min under 75 ℃.199Re-Pc1 was stable in CBS and PBS.RGD peptide had good binding-affinity to cancer cells(IC50=84.9 nmol/L).Its biodistribution showed that 188Re-Pc1 had a rapid blood clearance and was cleared mainly via the renal and hepatic route.188Re-Pc1 had high tumor uptake with a long time of tumor retention.更多还原