Ebastine依巴斯汀,90729-43-4

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Ebastine

CAS No. : 90729-43-4

MCE 国际站：Ebastine

产品活性：Ebastine (LAS-W 090) 是一种具有口服活性的第二代组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Ebastine 可用于过敏性鼻炎的症状和慢性特发性荨麻疹的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC.
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.

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.
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.

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