Lu, Jiayu; Wang, Xiangjun; Ge, Shuai; Hou, Yajing; Lv, Yuexin; He, Huaizhen; Wang, Cheng published the artcile< Synthesis and evaluation of new potential anti-pseudo-allergic agents>, Recommanded Product: 4-(4-Methoxyphenyl)-1-butanol, the main research area is anti pseudo allergy mubritinib MRGPRX2 receptor; B10-S; MRGPRX2; Mast cells; Mubritinib; Pseudo-allergy.
Pseudo-allergic reactions frequently occur following clin. drug use and sometimes even cause mortal danger. Mas-related G-protein-coupled receptor member X2 (MRGPRX2) is a novel receptor that mediates pseudo-allergy and is an important target in the treatment of allergies. However, to date, there are no synthetic small-mol. inhibitors that prevent anaphylactoid reactions through this pathway. Our preliminary research suggested that B10-S and mubritinib effectively inhibited LAD2 cells. Therefore, two novel derivatives were synthesized by integrating the active substructures of B10-S and mubritinib, according to the mol. docking results. The antiallergic inhibitory effects of the two compounds were preliminarily evaluated in vitro using β-hexosaminidase release, histamine release, and intracellular Ca2+ mobilization assays, and their binding sites on MRGPRX2 were analyzed by mol. docking. Both substances inhibited β-hexosaminidase and histamine release in LAD2 cells and decreased intracellular Ca2+ by inhibiting MRGPRX2 in MRGPRX2-HEK293 cells treated with C48/80 in a dose-dependent manner. The docking results suggested that the mols. could competitively bind to the active site on MRGPRX2 and Glu141, which were combined by C48/80. Our study indicated that the two compounds have potential anti-allergic properties, which may provide evidence that will facilitate the development of synthetic mols. with anti-pseudo-allergic activity for clin. use in the future.
Bioorganic & Medicinal Chemistry Letters published new progress about Allergy. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Recommanded Product: 4-(4-Methoxyphenyl)-1-butanol.
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Ether | (C2H5)2O – PubChem