尽管GLP-1有诸多优点,但临床开发最致命弱点是GLP-1在血液中的半衰期较短,主要原因有两个:一是因为被受体内二肽基肽酶4 (DPP-4) 以及中性肽链内切酶(NEP)所降解,两者的切割会使GLP-1失活。二是GLP-1在体内会被肾脏清除而快速降解,这使得内生GLP-1在体内的半衰期约为 2 min,且只有 10-15% 的GLP-1 完整...
Fujitani, Y., et al. 2009. Effects of exendin-4 on glucose tolerance, insulin secretion, and beta-cell proliferation depend on treatment dose, treatment duration and meal contents. Biochem Biophys Res Commun 390:809-814.
J., Wang, Y., et al. 2003. Impact of pramlintide on glucose fluctuations and postprandial glucose, glucagon, and triglyceride excursions among patients with type 1 diabetes intensively treated with insulin pumps. Diabetes Care 26:1-8.
J., Wang, Y., et al. 2003. Impact of pramlintide on glucose fluctuations and postprandial glucose, glucagon, and triglyceride excursions among patients with type 1 diabetes intensively treated with insulin pumps. Diabetes Care 26:1-8.
6.肠泌素: GLP1、GIP(原理直接促进Insulin/胰岛素分泌); 7.GLP类似物和GLP-1受体激动剂(原理直接促进Insulin/胰岛素分泌); 8.二肽基肽酶-4(DPP-4)抑制剂(原理间接促进Insulin/胰岛素分泌); 9.噻唑烷二酮类(原理增加身体细胞对葡萄糖的需求); 10.钠-葡萄糖协同转运...
GLP-1类多肽减肥药 最新的抗肥胖药物靶向GLP-1受体,胰高血糖素样肽-1 受体(GLP1R)是一种在胰腺 β 细胞和大脑神经元上发现的受体蛋白,它通过增强胰岛素分泌参与控制血糖水平。 胰高血糖素样肽1受体激动剂(GLP-1 receptor agonists, 简称GLP-1肽),通过增强β胰腺细胞分泌胰岛素和抑制α胰腺细胞释放胰高血糖素来...
胰岛素（Insulin）是人体中天然的降血糖物质，而胰高血糖素（Glucagon）则是升血糖物质，二者相互制衡，...
6. Joubert M, Opigez V, Pavlikova B, Peyro Saint Paul L, Jeandidier N, Briant AR, et al. Efficacy and safety of exenatide as add-on therapy for patients with type 2 diabetes with an intensive insulin regimen: A randomized double-blind trial. Diabetes, Obesity and Metabolism. 2021;23...
1.双胍类(原理减缓、减少葡萄糖被吸收进入血液,降低血液中葡萄糖的浓度和提高身体细胞对Insulin/胰岛素的敏感度); 2.甲型糖苷酶抑制剂(原理减缓、减少葡萄糖被吸收进入血液); 3.胰淀素类似物(原理减缓、减少葡萄糖被吸收进入血液); 4.硫酰基尿素类药物(原理直接促进Insulin/胰岛素分泌)); ...
[2] Kimball C., Murlin J. 1923. Aqueous extracts of pancreas III. Some precipitation reactions of insulin. J Biol Chem 58:337–348. [3] Zunz, E., La Barre, J. 1929. Contributiona a l'etude des variations physiologiques de la secretion interne du pancreas: Relations entre les secreti...