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新型糖尿病治疗药物exendin-4的研究进展 被引量：2

Recent progress on exendin-4,a novel therapeutic drug for diabetes
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摘要 Exendin-4(降血糖药)是首个在美国获准上市用于治疗2型糖尿病的肠促胰岛素拟似物。临床研究表明,其与二甲双胍、磺酰脲类药物、或噻唑烷二酮类药物合用,能有效地控制2型糖尿病患者的血糖。Exendin-4的作用机制包括葡萄糖依赖的促胰岛素分泌、抑制胰高血糖素分泌、增加β细胞质量、减缓胃排空和抑制食欲。近来还发现,exendin-4可增加胰岛移植受者的胰岛素分泌量。Exendin-4对中枢神经系统也有保护作用。本文对ex-endin-4的药理作用及其机制、药物特点等作一综述。 Exendin -4 is the first approved drug in the incretin mimetic class and is indicated for treatment of type 2 diabetes mellitus. Randomized trials have shown exendin- 4 to be efficacious in improving glycemic control when combined with either mefformin, a sulfonylurea, or a thiazolidinedione. Evidence suggests that the agent mechanisms may include glucose - dependent stimulation of insulin secretion, suppression of glucagon secretion, enhancement of β cell mass, slowing of gastric emptying and inhibition of food intake. Exendin -4 stimulates insulin secretion in islet transplant recipients. Last studies illustrate a potential protective role for exendin -4 in the central nervous systems. The article mainly reviews the pharmacological efficacy and its mechanisms of exendin -4, and contrasts exendin -4 actions with other antidiabetics.
作者 宋光明 申竹芳
机构地区 中国医学科学院、北京协和医学院药物研究所
出处 《中国临床药理学杂志》 CAS CSCD 北大核心 2008年第2期156-160,共5页 The Chinese Journal of Clinical Pharmacology
关键词 EXENDIN-4 肠促胰岛素拟似物 2型糖尿病 exendin - 4 incretin mimetic type 2 diabetes mellitus
分类号 R587.1 [医药卫生—内分泌] R977.15 [医药卫生—药品]
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参考文献38

  • 1Goke R, Fehmann HC, Linn T, et al. Exendin -d is a high potency agonist and truncated exendin- (9 - 39 ) -amide an antagonist at the glucagon -like peptide 1 - (7 - 36) -amide receptor of insulinsecreting beta-cells[J]. J Biol Chem, 1993; 268:19650-19655.
  • 2Greig NH, Holloway HW, De Ore KA, et al. Once daily injection of exendin - 4 to diabetic mice achieves long - term beneficial effects on blood glucose concentrations[J]. Diabetologia, 1999; 42:45-50.
  • 3Parkes DG, Pittner R, Jodka C, et al. Insulinotropic actions of exendin-4 and glucagon- like peptide- 1 in vivo and in vitro[ J]. Metabolism, 2001; 50:583 589.
  • 4Fehse F, trautmann M, Holst JJ, et al. Exenatide augments first - and second -phase insulin secretion in response to intravenous glucose in subjects with type 2 diabetes[ J]. J Clin Endoerinol Metab, 2005 ; 90: 5991 - 5997.
  • 5Moore MC, Cherrington AD. Regulation of net hepatic glucose uptake: interaction of neural and pancreatic mechanisms [ J ]. Reprod Nutr Dev, 1996; 36:399 406.
  • 6Kolterman OG, Buse JB, Fineman MS, et al. Synthetic exendin -4 (AC2993) significantly reduces postprandial and fasting plasma glucose in subjects with type 2 diabetes [ J ]. J Clin Endocrinol Metab , 2003; 88:3082 - 3089.
  • 7Dillon JS, Lu M, Bowen S, et al. The recombinant rat glucagon - like peptide- 1 receptor, expressed in an alpha- cell line, is coupled to adenylyl cyclase activation and intracellular calcium release [ J ]. Exp Clin Endocrinol Diabetes, 2005 ; 113 : 182 - 189.
  • 8Fehmann HC, Hering BJ, Wolf MJ, et al. The effects of glucagon - like peptide- Ⅰ (GLP -Ⅰ) on hormone secretion from isolated human pancreatic islets [ J ]. Pancreas, 1995 ; 11 : 196 - 200.
  • 9Green GM, Guan D, Schwartz JG, et al. Accelerated gastric emptying of glucose in Zucker type 2 diabetic rats : role in postprandial hyperglycaemia[J]. Diabetologia, 1997; 40:136 142.
  • 10Imeryuz N, Yegen BC, Bozkurt A, et al. Glucagon - like peptide - 1 inhibits gastric emptying via vagal afferent - mediated central mechanisms[J]. Am J Physiol, 1997; 273:920 - 927.

同被引文献38

  • 1黄静,徐进,左翼,徐伟东,吴自荣.重组人胰高血糖素样肽-1的表达及生物学活性[J].中国生物工程杂志,2006,26(1):50-55. 被引量：7
  • 2王小纯,祖向阳,张贵星.Exendin-4的研究进展[J].生命的化学,2007,27(4):334-336. 被引量：4
  • 3Nathan D.Long-team complication of diabetes mellitus.N Engl J Med.1993;328:1676-1684.
  • 4Diabetes Control and Complications Trial Research Group.The effect of intensive treatment of diabetes on the development of long-term complications in insulin-dependent diabetes mellitus.N Engl J Med.1993; 329:977-986.
  • 5Bloomgarden ZT.American diabetes Association postgraduate course, 1996: Treatment and prevention of diabetes.Diabetes Care.1996;19:784-786.
  • 6Sutherland DE, Gruessner AC, Gruessner RW.Pancreas transplantation: A review.Transplant Proc.1998;30: 1940-1943.
  • 7Fioretto P, Steffes MW, Sutherland DR, et al.Reversal of lesions of diabetic nephropathy after pancreas transplantation.N Engl J Med.1998;339(2):69-75.
  • 8Tyden G, Bolinder J, Solders G,et al.Improved survival in patients with insulin-dependent diabetes mellitus and end-stage diabetic nephropathy 10 years after combined pancreas and kidney transplantation.Transplantation.1999;67:645-648.
  • 9Shapiro AM, Lakey JR, Paty BW, et al.Strategic opportunities in c1inical islet transplantation.Transplantation.2005;79: 1304-1307.
  • 10Shapiro AM, Rieordi C, Hering BJ, et al.Internationa1 tria1 of the Edmonton Protocol for islet transplantation.N Engl J Med.2006;355:1318-1330.

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中国临床药理学杂志
2008年 第2期

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