Retatrutide, a synthetic peptide formulated by Eli Lilly, is also known as LY3437943. It consists of 39 amino acids and works by activating three receptors: GLP-1, GIP, and glucagon (GCG) [1]. Both GLP-1 and GIP belong to the incretin family of hormones that boost insulin secretion and influence immune responses. Activation of the GCG receptor is thought to enhance metabolic activity and stimulate energy use [2].
This novel compound is under investigation for its effectiveness in managing blood sugar and encouraging weight loss [3].
How Does Retatrutide Work?
Retatrutide operates by targeting GIP, GLP-1, and GCG receptors, with a significant emphasis on GIP receptor stimulation [4]. Incretin hormones like GLP-1 and GIP help in boosting insulin release from pancreatic beta cells and play a role in creating feelings of satiety. Glucagon counteracts low blood sugar by raising glucose levels during fasting. By engaging these receptors, retatrutide has a comprehensive effect on metabolic regulation, with notable impacts on both glucose control and body weight.
The peptide primarily acts by strongly activating the GIP receptor, which is pivotal for appetite regulation by affecting the brain’s centers responsible for fullness. This action helps reduce hunger, cravings, and food consumption [8].
Additionally, the GLP-1 receptor activation aids in controlling blood sugar and heightening satiety. GLP-1 further slows gastric emptying, leading to prolonged feelings of fullness post-meal [9, 10].
Through the stimulation of GCG receptors, retatrutide is believed to increase energy usage and support fat oxidation, particularly through liver metabolism. It may also induce the conversion of white fat to beige fat, increasing thermogenesis and boosting caloric expenditure [11].
These actions make retatrutide a promising candidate for research in obesity and type 2 diabetes management by not only limiting calorie intake but also enhancing energy use, offering a dual approach to effective weight management.
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