tBPC is a postitive allosteric modulator of the neuropeptide Y (NPY) Y4 receptor, which is predominantly expressed in the gastrointestinal tract and activated most strongly by pancreatic polypeptide (PP). tBPC was shown to potentiate Y4R activity in G-Protein signaling and arrestin3 recruitment and to potentiate the native PP response. tBPC was selective for Y4R over other Neuropeptide Y receptors and showed no effect on the efficacy (Emax) or potency (EC50) of the NPY signal response at the Y1, Y2, or Y5 receptors at 30 μM.
Journal of medicinal chemistry, 60(17), 7605-7612 (2017-08-11)
The human Y4 receptor (Y4R) and its cognate ligand, pancreatic polypeptide (PP), are involved in the regulation of energy expenditure, satiety, and food intake. This system represents a potential target for the treatment of metabolic diseases and has been extensively