Ebastine

Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research^[1]. In Vitro: Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC^[2].
Ebastine (10-500 ng/mL; 24-48 hours) treatment shows dose-dependent increases in Cyclin D1, Cyclin E1, and Cyclin A expression levels. And the expression levels of Cdk4, Cdk2, and Cdc2 are alos increased. Ebastine treatment elevates expression levels of phospho-AKT and phospho-p44/42 extracellular signal-regulated kinase^[2]. In Vivo: In rats, after intravenous administration of [¹⁴C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t_1/2 α) of 1.6 h and β-phase half-life (t_1/2 β) of 3.1 h^[3].
Following oral administration of [¹⁴C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (C_max) of 102 ng eq./ml at 2 h and decreased monophasically with t_1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with C_max of 1110 ng eq./ml at 4 h and with t_1/2 of 4.0 h^[3].