新型胰岛素促分泌剂rExendin-4体内药效学评价  

Pharmacodynamic evaluation of a new insulinotropic agent rExendin-4 in vivo

作　　者：环奕[1] 刘泉[1] 孙素娟[1] 王振基[1] 李平平[1] 陈跃腾[1] 申竹芳[1] 

机构地区：[1]中国医学科学院、北京协和医学院药物研究所中草药物质基础与资源利用教育部重点实验室,北京100050

出　　处：《中国临床药理学杂志》2010年第11期830-834,共5页The Chinese Journal of Clinical Pharmacology

基　　金：国家科技重大专项创新药物研究开发技术平台建设专项基金资助项目(2009ZX09301-003-12-1);十一五重大新药创制科技重大专项基金资助项目(2009ZX09303-003)

摘　　要：目的考察基因工程肽类rExendin-4(降血糖药)在正常ICR小鼠体内的药效学作用特征。方法选用正常ICR小鼠,考察rExendin-4对动物空腹血糖、糖负荷后血糖的变化、血清胰岛素水平以及胃肠蠕动的影响。结果 rEx-end in-4可以降低血糖,抑制糖负荷后血糖的升高;其促胰岛素分泌作用依赖于血糖升高的刺激,不伴随胰岛素引起的低血糖效应。结论 rExendin-4可安全有效的降低血糖,对糖尿病的防治具有良好的应用前景。Objective To identify the pharmacodynamics of a new genetic engineering peptide, rExendin -4, in normal ICR mice. Methods In normal ICR mice, observe rExendin -4＇s effects on blood glucose and serum insulin level, as well as blood glucose fluctuation after oral glucose load. Results The rExendin -4 shows benefitial blood glucose normalization, which dependents on the higher blood glucose stimulation and without hypoglycemia induced by insulin. It means to be a new insu- linotropic agent. Conclusion The rExendin -4 can effectively and safely achieve the ideal therapy target for type 2 diabetes mellltus with much less side effects such as hypoglycemia and weight gain, and possess favorable applieation perspective.

关 键 词：胰高血糖素样肽 促胰岛素分泌剂 2型糖尿病 

分 类 号：R962[医药卫生—药理学] R977.15[医药卫生—药学]