在大鼠中,GLP-1诱导的利钠和利尿伴随着肾血流量和肾小球滤过率增加[81,82],可能是GLP-1增加了肾入球小动脉的扩张而介导。肾脏去神经会导致GLP-1不能增加肾小球滤过率,降低GLP-1的利钠和利尿作用[81],这也表明GLP-1的利钠利尿作用可能是由于抑制近端小管的钠重吸收,并强调GLP-1需要完整的肾神经支配来增...
I.L., Woods, S.C., et al. 1998. Central infusion of glucagon-like peptide-1-(7-36) amide (GLP-1) receptor antagonist attenuates lithium chloride-induced c-Fos induction in rat brainstem. Brain Res 801:164-170.
GLP-1的全称是胰高血糖素样肽-1(glucagon-like peptide 1),是1983年发现的一种小肠分泌、可以进入循环系统到达胰腺、促进胰腺分泌胰岛素的多肽激素,由30个氨基酸构成[1]。但GLP-1这种激素的体内半衰期极短,只有2-5分钟,无法真正成药。自新世纪之后,诺和诺德公司和美国礼来公司才通过各种化学修饰(引入非天然氨基酸,...
GLP-1 receptor antagonistDipeptidyl-peptidase 4 inhibitorDiabetesTreatmentCardiovascular diseaseIncretin-based pharmacotherapyIncretin-based therapy became recently available as antihyperglycemic treatment for patients with type 2 diabetes (T2DM). Incretin therapy comprises glucagon-like peptide receptor agonists (...
MoA:GLP-1 agonist + GIP antagonist Company:AmGen CT-388 Brand Name:n/a MoA:GIP/GLP Glucagon receptor agonist Company:Carmot Therapeutics CT-868 Brand Name:n/a MoA:GIP/GLP Glucagon receptor agonist Company:Carmot Therapeutics GSBR-1290
both on its own and after the consumption of a mixed-nutrient drink in healthy men. However, the contribution of GLP-1 to insulin stimulation was likely modest, and further evaluation using a GLP-1 receptor antagonist would be necessary. Additionally, studies in patients with T2DM are now need...
Glucagon like Peptide 1 (GLP-1) analogs and sulfonyurea drugs are used clinically to enhance pancreatic β-cell function and treat diabetes. However, rapid degradation and off-target effects limit their usefulness. Here we describe an approach for targeting β-cells by synthesizing a bi-...
Intravenous exenatide improved fasting EF, an effect nullified by exendin-9 (GLP-1R antagonist). Exenatide activated eNOS and NO production in endothelial cells, induced dose-dependent vasorelaxation, and mitigated high-glucose or lipid-induced endothelial dysfunction in arterioles ex vivo, effects which...
About Avexitide Avexitide is an investigational, first-in-class glucagon-like peptide-1 (GLP-1) receptor antagonist that has been evaluated in five Phase 2 clinical studies for post-bariatric hypoglycemia (PBH) and has also been studied in congenital hyperinsulinism (HI), with U.S. Food ...
the current standard of care (SOC), and raised concerns about the illicit use of opioid medications, known as ‘diversion’. The risk of diversion is not confined to methadone, and certain formulations of buprenorphine have naloxone (an opioid antagonist) added to their formulation in order to ...