产品描述:
Ebastine is a histamine H1 receptor antagonist and prodrug form of carebastine (Item No. 23076).{24985} Ebastine binds to histamine H1 receptors with an IC50 value of 45 nM. It is selective for histamine H1 receptors over α1-adrenergic and muscarinic M1 and M2 receptors (IC50s = 183, 1,100, and >10,000 nM, respectively), as well as dopamine D2 receptors and the serotonin (5-HT) receptor subtype 5-HT1A at 1 and 10 µM, respectively.{24986} Ebastine (1, 5, and 10 µM) inhibits T cell proliferation and the production of IL-4 and IL-5 in isolated human T cells.{24987} It also reduces phytohemagglutinin-induced T cell migration and decreases LPS-induced IL-6 and TNF-α production by macrophages isolated from peripheral blood mononuclear cells (PBMCs). Ebastine inhibits histamine-induced and allergen-induced bronchospasm in guinea pigs (ED50s = 115 and 334 µg/kg, respectively).{47108} Formulations containing ebastine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.