GLP_1受体激动剂及DPP_抑制剂的研究进展.pdf

学 报 Journal of China Pharm aceuticalUn iversity 2008, 39( 5): 385- 391 385 药学前沿 GLP1受体激动剂及 DPP 抑制剂的研究进展 * 周映红, 黄文龙 , 张惠斌, 迟玉石 (中国药科大学新药研究中心, 南京 210009) 摘 要 对糖尿 病治疗药胰高血糖素样肽 1( G LP1)受体激动剂和二肽基肽酶 ( DPP ) 抑制剂的研究进展进 行了 综述。介绍了 G LP1的血糖调控机制, 还对 GLP1受体激动剂 ( 如 Ex endin4, Exentide LAR, L irag lutide, C JC1131, 非 肽类 GL P1受体激动剂 ) 和 DPP 抑制剂 ( 如 Sitag liptin, V ildag liptin, Saxag liptin, A log liptin) 进 行了详 细的介 绍, 为 2型糖 尿病 治疗药物的研发提供 参考。 关键词 胰高血 糖素样肽 1; 胰高 血糖素样肽 1受体; 二肽基肽酶 ( D PP ); 2型糖尿病 中图分类号 R587. 1; R 782. 4 文献标识码 A 文章编号 1000- 5048( 2008) 05- 0385- 07 Progress in the investigation of GLP1 receptor agonists and DPP inhibitors ZHOU Y inghong, HUANG W enlong* , ZHANG H u ibin, CH I Yushi Center of D rug D iscovery; China Pharm aceutical Un iversity, N anjing 210009, China Abstract The research advances of glucagon- like peptide1 (GLP1) receptor agonists and dipeptidy l pepti dase IV (DPPIV) inhibitors are rev iew ed in this paper and the pharm aco log ica lm echanism o f GLP1 in blood glucose regu lation is also presented. M oreover, GLP1 receptor agonists ( such as Exendin4, Exentide LAR, L ira glutide, C JC1131, a nonpeptidic GLP1 receptor agonist) and DPPIV inh ibitors ( S itag liptin, V ildag liptin, Saxa gliptin, and A log liptin) are a lso introduced in deta i,l a im s at prov id ing references for the research and develop m ent o f agents for the treatm ent o f type 2 d iabetes. Key words g lucagonlike peptide1( GLP1); glucagonlike peptide1 receptor; dipeptidy l peptidase IV; type 2 diabetes 胰高血糖素样肽 1( g lucagonlike peptide1 re 的危险; 二是阻止胰腺 细胞退化, 刺激 细胞的 ceptor, GLP1)受体属于