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tBPC is a selective positive allosteric modulator for human Y4 receptor (Y4R), which enhances the activation of Y4R in G protein signaling and arrestin3 recruitment[1].

tBPC is a postitive allosteric modulator of the neuropeptide Y (NPY) Y4 receptorwhich 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 Y1Y2or Y5 receptors at 30 μM.

[1] Schubert M, et al., Identification and Characterization of the First Selective Y4 Receptor Positive Allosteric Modulator. J Med Chem. 2017 Sep 14;60(17):7605-7612. DOI:10.1021/acs.jmedchem.7b00976