化学合成两类去唾液酸糖蛋白受体（ＡＳＧＰＲ）的人工配体———半乳糖基白蛋白（ＧａｌｎＨＳＡ）和半乳糖基多聚Ｌ谷氨酸（ＧａｌｎＰＬＧＡ），并以１２５Ｉ标记的去唾液酸胎球蛋白（ＡＳＦ）为标准配体，测定了合成配体抑制１２５ＩＡＳＦ与大鼠肝细胞膜ＡＳＧＰＲ结合的ＩＣ５０值．结果表明，Ｇａｌ１２ＨＳＡ、Ｇａｌ１５ＨＳＡ、Ｇａｌ２６ＨＳＡ、Ｇａｌ３０ＨＳＡ和Ｇａｌ３４ＰＬＧＡ均能够有效地抑制１２５ＩＡＳＦ与ＡＳＧＰＲ的结合，且前者与ＡＳＧＰＲ的亲和力随半乳糖基化程度的增加而增加．这些合成配体来源丰富、制备简单，适合于作为药物或基因肝靶向运送的导向配体． Two synthetic artificial ligands for asialoglycoprotein receptor (ASGPR), GalnHSA and GalnPLGA, were chemically synthesized and labeled with 125I Asialoflagulin (ASF) was used as a standard ligand to determine the IC50 value of the synthetic ligand for inhibiting the binding of 125I-ASF to the rat hepatocyte membrane ASGPR. The results showed that both Gal12HSA, Gal15HSA, Gal26HSA, Gal30HSA and Gal34PLGA could effectively inhibit the binding of 125I-ASF to ASGPR, and the affinity of AS12PR with ASGPR increased with the increase of galactosylation. These synthetic ligands are abundant in origin, simple to prepare and suitable as targeting ligands for drug or gene liver targeted delivery.