在体外已经证实了KATP通道活性在介导GLP-1释放中的重要性,同时也证实人L-细胞中存在KATP通道的Kir6.2/SUR1通道复合物[31],但KATP通道的Kir6.2/SUR1通道复合物是否在人体中介导GLP-1释放这一过程的作用还有待证实。 图2 L-细胞内营养物质刺激GLP-1分泌的示意图 CICR:钙诱导的钙释放;LCFA:长链脂肪酸;GLUT2:葡...
GIP刺激迷走神经传入传递,随后激活迷走传出神经元和肠神经元,释放乙酰胆碱和/或GRP来刺激远端肠道释放GLP-1,触发GLP-1分泌,而营养物质如能到达远端肠道时,与L-细胞的直接接触也会触发GLP-1分泌进入循环。 02 中枢GLP-1分泌的内分...
GIP刺激迷走神经传入传递,随后激活迷走传出神经元和肠神经元,释放乙酰胆碱和/或GRP来刺激远端肠道释放GLP-1,触发GLP-1分泌,而营养物质如能到达远端肠道时,与L-细胞的直接接触也会触发GLP-1分泌进入循环。 02 中枢GLP-1分泌的内分泌调节 后脑孤束核(NTS)尾部的的GCG+神经元是内源性脑GLP-1的主要来源[71]。NT...
Cornell S. A review of GLP-1 receptor agonists in type 2 diabetes: A focus on the mechanism of action of once-weekly agents. J Clin Pharm Ther. 2020 Sep;45 Suppl 1(Suppl 1):17-27. Shah M, Vella A. Effects of GLP-1...
Malendowicz, L.K., Nussdorfer, G.G., Nowak, K.W., Ziolkowska, A., Tortorella, C., Trejter, M. 2003. Exendin-4, a GLP-1 receptor agonist, stimulates pituitary-adrenocortical axis in the rat: Investigations into the mechanism(s) underlying Ex4 effect. Int J Mol Med 12:237-241...
[2] Fujita, Hiroki, et al. "The protective roles of GLP-1R signaling in diabetic nephropathy: possible mechanism and therapeutic potential." Kidney international 85.3 (2014): 579-589.[3] Pabreja, Kavita, et al. "Molecular mechanisms underlying physiological and receptor pleiotropic effects ...
尽管GLP-1R激动剂以其促胰岛素和降低体重的作用而闻名,但它也对啮齿动物的心血管系统产生一系列有益的作用,包括通过抑制心肌细胞凋亡来增加心肌细胞存活,改善内皮功能障碍[8,11],改善损伤和心力衰竭后的局部和总心输出量[12-15](图1)。高血压患者也有血压降低的报道[16]。延长利拉鲁肽治疗时间可进一步改善T2DM患...
With regard to their effects on body weight, the principal action of GLP-1 agonists is mediated via their inhibition of eating. In searching for the underlying mechanism of GLP-1 receptor agonist-induced anorexic effect, scientists have discovered pathways in the central nervous system, as well ...
[3] Meloni AR, DeYoung MB, Lowe C, Parkes DG. GLP-1 receptor activated insulin secretion from pancreatic β-cells: mechanism and glucose dependence. Diabetes Obes Metab. 2013 Jan;15(1):15-27. [4] Rameshrad M, Razavi BM, Lalau JD, De Broe ME, Hosseinzadeh H. An overview of glucago...
药物靶点作用机制在研适应症药物最高研发状态(全球)药物类型在研机构GMA102/105(重组抗人GLP-1受体人源化单克隆抗体)GIP-1RGIP-1R激动剂2型糖尿病;肥胖;超重临床3期单克隆抗体鸿运华宁(杭州)生物医药有限公司(Gmax Biopharm LLC)Recombinant GLP-1 receptor agonists (Beijing Lepu)(重组GLP-1受体激动剂GIP-1RG...