ML382 is a potent (EC 50 = 190 nM in the presence of the endogenous peptide MRGX1 agonist BAM8-22) and selective positive allosteric modulator of the Mas-related G protein-coupled receptor X1 (MRGX1 or MRGPRX1), a receptor whose expression is limited to subsets of small-diameter sensory neurons...
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ML382 is a potent (EC 50 = 190 nM in the presence of the endogenous peptide MRGX1 agonist BAM8-22) and selective positive allosteric modulator of the Mas-related G protein-coupled receptor X1 (MRGX1 or MRGPRX1), a receptor whose expression is limited to subsets of small-diameter sensory neurons in dorsal root ganglia and trigeminal neurons. ML382 significantly enhanced the antihyperalgesic effects of exogenously added BAM8-22 and in mouse models of persistent pain without exogenous BAM8-22, suggesting enhanced pain inhibition from a sufficient supply of endogenous MRGPRX1 ligands and a potential new pain therapeutic
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