含RGD序列多肽的<sup>188</sup>Re标记及其生物分布

含RGD序列多肽的¹⁸⁸Re标记及其生物分布

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U87MG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。

Abstract: A cyclic RGD containing peptide H-c(RGDyK) (Pc1) was labeled with ¹⁸⁸Re using fac-¹⁸⁸Re(CO)₃(H₂O)₃as 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.