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.
tBPC是一种具有选择性的Y4受体正向变构调节剂。tBPC可增强Y4受体在G蛋白信号传导和arrestin3招募中的激活作用来增强胰腺多肽、神经肽Y和肽YY的Y4R反应，同时通过选择性调节Y4受体而不影响Y1、Y2或Y5受体以维持特异性[1]。
在体外，tBPC（5.1μM-30μM）处理COS7细胞和HEK293细胞30分钟。tBPC处理能增强Polypeptide和其它肽段（NPY，PYY）对Y4R的激活效应，和arrestin3招募速率[1]。