Lodoxamide

Lodoxamide is a potent agonist of GPR35 with an EC50 value 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 (Item No. 22173), anti-IgE, or A23187 (Item No. 11016) 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.