ML382 is a positive allosteric modulator of Mas-related G-protein-coupled receptor X1 (MrgprX1, MrgX1, SNSR4), a G-protein coupled receptor (GPCR) selectively expressed in dorsal root ganglion (DRG) neurons. MrgX1 is believed to be a functional ortholog of mouse MrgC11, which has been shown to be involved in itch and pain. ML382 is selective for MrgX1 over MrgX2, MrgC11 and a panel of 68 other GPCRs, ion channels and transporters, with an EC50 value of 190 nm with an Emax value of 148% in the presence of the known ligand BAM8-22.
Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1
ChemMedChem, 10, 57-61 (2015)
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