According to their pharmacodynamics and pharmacokinetic properties, the GLP-1RAs are categorized as either short-acting or long-acting agents. Short-acting GLP-1RAs, such as exenatide and lixisenatide, have a half-life of 2–4 h, requiring daily administration once or twice a day. Long-acting ...
According to their pharmacodynamics and pharmacokinetic properties, the GLP-1RAs are categorized as either short-acting or long-acting agents. Short-acting GLP-1RAs, such as exenatide and lixisenatide, have a half-life of 2–4 h, requiring daily administration once or twice a day. Long-acting ...
To accomplish that, a high-affinity GPCR ligand (agonist or antagonist) is usually added to the extracellular side to shift the equilibrium to either the active or inactive state. At the intracellular side, G protein/mini-G protein/nanobody has recently been used to stabilize the GPCR active ...
Many in vivo and in vitro studies make use of Ex-4, a well-known orthosteric antagonist for the GLP-1R [27]. It should come as no surprise that GLP-1 has pleiotropic effects beyond reducing glucose levels, considering the widespread distribution of GLP-1R. Among these effects are those ...
Experiment 1c: food intake following HPFv GLP-1R anta- gonist, exendin-(9–39). Rats (n ¼ 9; avg. BW ¼ 334 g) received bilateral injections of 0, 1.25, 2.5, or 5 mg exendin-(9–39) (total doses: 2.5 mg, 5 mg, 10 mg), a selective GLP-1R antagonist, to the HPFv ...
A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings Article Open access 05 February 2024 Development of an orally delivered GLP-1 receptor agonist through peptide engineering and drug delivery to treat chronic dis...
Fig. 1 Examples of CMR sequences used to evaluate cardiovascular effects of SGLT2i or GLP-1Ra. ECV: extracellular volume; MRS: magnetic resonance spectroscopy; LGE: late gadolinium enhancement; STIR-T2: Short-TI Inversion Recovery Full size image ...
Thus, N-terminally extended GLP-1 (PG 72-107)amide is inactive and appropriate doses of the GLP-1 antagonist, exendin 9-39, abolish the effects of GLP-1 (41). Acute, peripheral administration of GLP-1 does not inhibit food intake acutely in rats (41, 42). However, it remains ...
Pat. No. 6,864,069 as acting as both a GLP-1 agonist and a glucagon antagonist for treating diabetes are also excluded as glucagon/GLP-1 co-agonist molecules. In another embodiment, excluded is the use of glucagon antagonists to treat diabetes, such as the antagonists described in Unson ...
(alone or in combination with another GLP-1R agonist, e.g., liraglutide, exenatide, dulaglutide, albiglutide, lixisenatide, or semaglutide), a peroxisome proliferator-activated receptor alpha (PPARα) agonist, fish oil, an acetyl-coA carboxylase (ACC) inhibitor, a TGFβ antagonist, GFRAL agonist...