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.
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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
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