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Free Fatty Acid Receptor 1 (FFAR1) is a G-protein-coupled receptor that acts as a metabolic sensor for circulating free fatty acids. It is highly expressed in pancreatic β-cells, where it modulates insulin secretion in response to elevated glucose levels. Activation of FFAR1 enhances glucose-stimulated insulin secretion and stimulates incretin hormone release. Central pharmacological activation may offer therapeutic potential against obesity by increasing energy expenditure and reducing inflammation/stress responses within the hypothalamus. Synthetic agonists like TAK-875 have been developed for diabetes treatment but faced challenges related to safety profiles during clinical development.
Agonist of FFAR1, enhances glucose-stimulated insulin secretion from pancreatic β-cells
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