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As a triple incretin receptor agonist, it: Activates GLP-1 receptors , reducing appetite, slowing gastric emptying, and improving insulin secretion Activates GIP receptors , enhancing insulin response and potentially supporting fat metabolism Activates glucagon receptors , increasing energy expenditure and hepatic glucose output Whilst glucagon receptor activation increases hepatic glucose output, the net glycaemic effect of retatrutide is mitigated by the concurrent GLP-1 and GIP activity, resulting in overall improvements in glycaemic control in trial participants

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The peptide functions by binding to melanocortin receptors, leading to increased melanin synthesis in the skin