tBPC is a selective positive allosteric modulator of the Y4 receptor. tBPC enhances the activation of the Y4 receptor in G protein signaling and arrestin3 recruitment, thereby potentiating the Y4R responses to pancreatic polypeptide, neuropeptide Y, and peptide YY, while maintaining specificity by selectively modulating the Y4 receptor without affecting the Y1, Y2, or Y5 receptors[1].
In vitro, treatment of COS7 cells and HEK293 cells with tBPC (5.1μM-30μM) for 30 minutes enhances the activation effect of Polypeptide and other peptides (NPY, PYY) on Y4R, as well as the rate of arrestin3 recruitment[1].
References:
[1] Schubert M, Stichel J, Du Y, et al. Identification and Characterization of the First Selective Y4 Receptor Positive Allosteric Modulator. J Med Chem. 2017 Sep 14;60(17):7605-7612.