Lodoxamide (U-42585E; Alomide) is an antiallergic agent acting as a mast cell stabilizer, as well as a potent agonist of GPR35 with an EC50 of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor. It inhibits histamine release induced by compound 48/80, anti-IgE, or A23187 in isolated rat peritoneal mast cells (IC50s = 0.1-50 μM) and inhibits A23187-induced calcium influx in mast cells. It reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 μg/ml. Lodoxamine (0.1 and 10%, w/v) reduces the immediate hypersensitivity response in rat conjunctiva in vivo in a dose-dependent manner and reduces mast cell degranulation in a topical ovalbumin challenge. Formulations containing lodoxamide have been used in the treatment of vernal conjunctivitis and keratitis.
理化性质和储存条件
Molecular Formula: C11H6ClN3O6;
Exact Mass: 310.9945
Molecular Weight: 311.63
Synonym: Lodoxamidum; U-42585E; U42585E; U-42585-E; Lodoxamida;
Chemical Name:2,2'-((2-chloro-5-cyano-1,3-phenylene)bis(azanediyl))bis(2-oxoacetic acid)
InChi Key:RVGLGHVJXCETIO-UHFFFAOYSA-N
InChi Code:InChI=1S/C11H6ClN3O6/c12-7-5(14-8(16)10(18)19)1-4(3-13)2-6(7)15-9(17)11(20)21/h1-2H,(H,14,16)(H,15,17)(H,18,19)(H,20,21)
SMILES Code:N#CC1=CC(NC(C(O)=O)=O)=C(Cl)C(NC(C(O)=O)=O)=C1
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