ML382
MRGPRX1 positive allosteric modulator / ML382 is a potent (EC50 = 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.1 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.2
Biochemicals & reagents
1646499-97-9
VU0485891; 2-(Cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide
1) Wen, et al. (2015), Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1; ChemMedChem.. 10 57 2) Li, et al. (2017), Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain; Proc. Natl. Acad. Sci. USA. 114 E1996
-20°C
TARGET: GPCR -- PATHWAY: Cation channel -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain