Department of Cardiology, University Medical Centre of the Johannes Gutenberg University, Mainz, Germany.
Center of Thrombosis and Hemostasis (CTH), University Medical Center, Mainz, Germany.
Br J Pharmacol. 2022 Feb;179(4):659-676. doi: 10.1111/bph.15462. Epub 2021 May 6.
Cardiovascular outcome trials revealed cardiovascular benefits for type 2 diabetes mellitus patients when treated with long-acting glucagon-like peptide-1 (GLP-1) receptor agonists. In the last decade, major advances were made characterising the physiological effects of GLP-1 and its action on numerous targets including brain, liver, kidney, heart and blood vessels. However, the effects of GLP-1 and receptor agonists, and the GLP-1 receptor on the cardiovascular system have not been fully elucidated. We compare results from cardiovascular outcome trials of GLP-1 receptor agonists and review pleiotropic clinical and preclinical data concerning cardiovascular protection beyond glycaemic control. We address current knowledge on GLP-1 and receptor agonist actions on the heart, vasculature, inflammatory cells and platelets, and discuss evidence for GLP-1 receptor-dependent versus independent effects secondary of GLP-1 metabolites. We conclude that the favourable cardiovascular profile of GLP-1 receptor agonists might expand their therapeutic use for treating cardiovascular disease even in non-diabetic populations. LINKED ARTICLES: This article is part of a themed issue on GLP1 receptor ligands (BJP 75th Anniversary). To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.4/issuetoc.
心血管结局试验显示,2 型糖尿病患者接受长效胰高血糖素样肽-1(GLP-1)受体激动剂治疗可带来心血管获益。在过去十年中,人们在描述 GLP-1 的生理作用及其对包括大脑、肝脏、肾脏、心脏和血管在内的众多靶标的作用方面取得了重大进展。然而,GLP-1 及其受体激动剂和 GLP-1 受体对心血管系统的影响尚未完全阐明。我们比较了 GLP-1 受体激动剂心血管结局试验的结果,并回顾了有关除血糖控制以外的心血管保护的多种临床和临床前数据。我们讨论了当前关于 GLP-1 和受体激动剂对心脏、血管、炎性细胞和血小板作用的知识,并讨论了 GLP-1 代谢物的 GLP-1 受体依赖性和非依赖性作用的证据。我们的结论是,GLP-1 受体激动剂有利的心血管特征可能会扩大它们在治疗心血管疾病方面的治疗用途,即使在非糖尿病人群中也是如此。 相关文章:本文是关于 GLP1 受体配体的专题(BJP 75 周年纪念)的一部分。要查看本节中的其他文章,请访问 http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.4/issuetoc.