| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| 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 (t1/2 α) of 1.6 h and β-phase half-life (t1/2 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 (Cmax) of 102 ng eq./ml at 2 h and decreased monophasically with t1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with Cmax of 1110 ng eq./ml at 4 h and with t1/2 of 4.0 h[3]. | ||||||||||||
| Name | Ebastine | ||||||||||||
| CAS | 90729-43-4 | ||||||||||||
| Formula | C32H39NO2 | ||||||||||||
| Molar Mass | 469.66 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. J Sastre. Ebastine in allergic rhinitis and chronic idiopathic urticarial. Allergy. 2008 Dec;63 Suppl 89:1-20. [2]. Fu-Ming Tsai, et al. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503. [3]. Fujii, et al. Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats. Arzneimittelforschung. 1994 Apr;44(4):527-38. |