Lithocholic Acid Activates Mas-Related G Protein-Coupled Receptors, Contributing to Itch in Mice.

ABSTRACT: The present study focused on lithocholic acid (LCA), a secondary bile acid that contributes to cholestatic pruritus. Although recent studies have found that LCA acts on MAS-related G protein-coupled receptor family member X4 (MRGPRX4) in humans, it is unclear which subtypes of MRGPRs are activated by LCA in mice since there is no precise ortholog of human MRGPRX4 in the mouse genome. Using calcium imaging, we found that LCA could activate mouse Mrgpra1 when transiently expressed in HEK293T cells. Moreover, LCA similarly activates mouse Mrgprb2. Importantly, LCA-induced responses showed dose-dependent effects through Mrgpra1 and Mrgprb2. Moreover, treatment with QWF (an antagonist of Mrgpra1 and Mrgprb2), YM254890 (Gα_q inhibitor), and U73122 (an inhibitor of phospholipase C) sign

SUBMITTER: Song MH 

PROVIDER: S-EPMC8724838 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature