GLP-1 medications bind to GLP receptors to trigger the effects (or roles) of the GLP-1 hormone. The higher the dose of the GLP-1 agonist, the more extreme
临床前数据表明,相较于单独GLP-1类似物或单独雌激素,GLP-1/雌激素结合产物可增强小鼠厌食、减重、促胰岛素和胰岛保存作用[83-85]。而这种GLP-1/雌激素结合物并没有雌激素独有的促子宫内膜增生的效应,仅体现GLP-1成分介导的治疗指标改善。GLP-1R靶向作用也...
amide进行药物开发，而这两种天然的 GLP-1RA 会很快被DPP-4酶解，并在 1-2 min 内被肾脏清除，不具...
GLP-1能缓冲胰高糖素的高血糖效应,同时GLP-1抑制食欲与胰高糖素的能量消耗作用相协同以降低体重。将GLP-1和胰高糖素联合输注给人类受试者可导致食物摄入减少、能量消耗增加,提示这是由GLP-1联合胰高糖素作用所致[50,51]。与单激动剂相比,长期给非人类灵长类肥胖动物使用选择性双激动剂,体重可明显减轻[52]。
之前上海瑞金医院的王卫庆教授在本刊通过两篇文章为大家介绍了多肽类药物如何突破壁垒成为口服多肽(详见本刊2021年12月10日“ ”篇),以及司美格鲁肽如何在SNAC的助力下从注射制剂成为全球第一个真正意义上的口服肽类药物[即第一个口服给药的胰高糖素样肽-1受体激动剂(GLP-1RA)](详见本刊2022年1月14日“ ”...
之前上海瑞金医院的王卫庆教授在本刊通过两篇文章为大家介绍了多肽类药物如何突破壁垒成为口服多肽(详见本刊2021年12月10日“口服多肽,曙光初现”篇),以及司美格鲁肽如何在SNAC的助力下从注射制剂成为全球第一个真正意义上的口服肽类药物[即第一个口服给...
Mazdutide is a once-weekly glucagon-like peptide-1 (GLP-1) and glucagon receptor dual agonist. We evaluated the efficacy and safety of 24-week treatment of mazdutide up to 6 mg in Chinese overweight adults or adults with obesity, as an interim analysis of a randomised, two-part (low...
Guided by our results indicating an increased anxiety-like behavior after central GLP-1R agonist application and increased serotonin turnover in the amygdala, but not the hippocampus, we hypothesized that the anxiogenic effects of GLP-1 may originate from direct DR GLP-1R activation. The results ...
To summarize current knowledge about GLP-1 receptor agonist. Major conclusions At present, GLP-1 RAs are injected twice daily (exenatide b.i.d.), once daily (lixisenatide and liraglutide), or once weekly (exenatide once weekly, dulaglutide, albiglutide, and semaglutide). A daily oral preparation...
This review discusses current considerations for GLP-1 receptor agonist use in patients with T2D and DKD. Keywords: albuminuria; atherosclerotic cardiovascular disease; dulaglutide; exenatide; lixisenatide; liraglutide; semaglutide1. Introduction The number of people living with diabetes (DM) continues to ...