Oxatomide

Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases^[1][2][3][4]. In Vitro:Oxatomide (1-30 μM; 0-60 s) inhibits the elevation of [Ca²⁺]i induced by 1 mM ATP in N18TG2 cells, with an IC₅₀ of 3.37 μM^[1].
Oxatomide (10 μM; pre-treatment) inhibits the phosphorylation of ERK and p38 MAPK induced by ATP in N18TG2 cells^[1].
Oxatomide (10 μM; pre-treatment) inhibits the upregulation of COX-2 and MIP-2 mRNA and the secretion of MIP-2 induced by BzATP in J774 macrophages^[1].
Oxatomide (0-30 μM; 0-48 h) can promote the apoptosis of peripheral blood eosinophils and inhibit the survival induced by IL-5^[2].
Oxatomide (0.1-10 μM; 15 min) inhibits the immunological release of histamine and LTC₄ in human basophils^[3].
Oxatomide (0.1-10 μM; 15 min) inhibits the release of histamine, tryptase and PGD₂ after stimulation by anti-IgE or anti-FcεRI in human skin mast cells^[3]. In Vivo:Oxatomide (5-30 mg/kg; oral gavage; 5 days-2 weeks) has a beneficial effect in the chinchilla model of immune-mediated exudative otitis media^[4].