然而,要将GLP-1应用于临床也面临着问题,即人体自身产生的GLP-1极易被体内的二肽基肽酶Ⅳ(DPP-4)降解,其血浆半衰期不足2分钟,必须持续静脉滴注或持续皮下注射才能产生疗效,这大大限制了GLP-1的临床应用。 (来源;http://pdb101.rcsb.org/...
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...
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加肾小球滤过。在啮齿动物和人的研究中表明GLP-1R在肾血管系统中表达[88]。GLP-1、exendin-4和DPP-4抑制剂西格列汀降低大鼠[...
具有改善的药理学和药物递送特性的GLP-1受体激动剂.pdf,公开了可用于活化胰高血糖素样肽‑1(GLP‑1)受体并治疗或预防至少部分由胰高血糖素样肽1(GLP‑1)介导的疾病或病症的多肽、组合物和方法。(19)国家知识产权局 (12)发明专利申请 (10)申请公布号 CN 118076367 A (4
[27]Zinman B, Bhosekar V, Busch R, Holst I, Ludvik B, Thielke D, Thrasher J, Woo V, Philis-Tsimikas A. Semaglutide once weekly as add-on to SGLT-2 inhibitor therapy in type 2 diabetes (SUSTAIN 9): a randomised, placebo-controlled trial. Lance...
2型糖尿病;心血管事件;钠葡萄糖协同转运蛋白2抑制剂;胰高血糖素样肽-1受体激动剂 Research advance in SGLT2 inhibitor combined with GLP-1 receptor agonist in the treatment of type 2 diabetes with cardiovascular disease ZHAO Zhe, YANG Dandan, ZHAN Xiaorong (Third Department of Endocrinology, First ...
主要内容 123 肠促胰素治疗的发展历程 肠促胰素治疗药物的分类及特点 肠促胰素治疗药物的差别 基于肠促胰素治疗的发展经历了80多年时间 GLP-1被发现发展为治疗2型糖尿病的药物确定促胰岛素分泌的效应定义肠促胰素肠促胰素及肠－胰素轴进一步被定义 命名‘肠－胰素轴’193019601970 发现exendin-4 肠促胰素治疗临床...
These effects were significantly attenuated by GLP-1, forskolin (a cAMP activator) and Y-27632 (a ROCK2 inhibitor). However, H89 (a PKA inhibitor) inhibited the action of GLP-1, both in terms of inhibition of RASMC proliferation and migration, and RHOA/ROCK2 expression. These results ...
“therapy should begin with lifestyle management and metformin and subsequently incorporate an agent proven to reduce major cardiovascular events and cardiovascular mortality (currently empagliflozin [an SGLT-2 Inhibitor] and liraglutide [a GLP-1]), after considering drug-specific and pat...
eGFR, estimated glomerular filtration rate; HbA1c, hemoglobin A1c; ACE/ARB, angiotensin converting enzyme inhibitors/angiotensin-receptor blockers Postop, Postprocedural; GLP-1RA, glucagon-like peptide-1 receptor agonist; DPP4i, dipeptidyl peptidase-4 inhibitor; SGLT2i, sodium-glucose co-transporter-...