Tirzepatide is a dual agonist for the glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 receptors, designed to combine incretin hormone actions in a single peptide framework. In preclinical models, tirzepatide activates both receptors with high affinity, triggering cAMP-mediated signaling, insulinotropic activity, and coordinated effects on metabolic tissues. Mechanistic studies in rodents and in vitro systems suggest additive or synergistic modulation of appetite, lipid metabolism, and energy expenditure when compared to single-pathway agonists. This dual incretin approach has been extensively studied in receptor pharmacology experiments to dissect the contributions of GIPR and GLP-1R to metabolic regulation in laboratory settings.
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