化合物 Fenspiride T60417

Product Introduction
Bioactivity


英文名: Fenspiride

描述: Fenspiride 是 H1-组胺受体的拮抗剂。 Fenspiride 是一种具有口服活性的非甾体类抗炎药，可用于治疗呼吸道感染和中耳炎。 Fenspiride 抑制磷酸二酯酶 4 和磷酸二酯酶 3 的活性，-logIC50 值分别为 4.16+/-0.09 和 3.44+/-0.12。 磷酸二酯酶 5 活性也受到抑制，-logIC50 值约为 3.8。

体外活性: Fenspiride (approximately 100 μM) inhibits histamine-induced tracheal constriction in the isolated guinea pig. Fenspiride (< or = 10(-3) M) produced less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities [2].

体内活性: Administered orally at 60 mg/kg for 3 days, Fenspiride reduced the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum (4.2 + 0.9 vs. 2.3 + 0.5 ng/ml, P < 0.05) and in the bronchoalveolar lavage fluid (55.7 + 20 vs. 19.7 + 7.5 ng/ml, P < 0.05) of the model of endotoxemia that also reduced the lipopolysaccharide-induced primed stimulation of alveolar macrophages [3]. Administered orally at 60 mg/kg for 3 days, Fenspiride reduced the increased serum concentrations of extracellular type II phospholipase A 2, the intensity of the neutrophilic alveolar invasion, and the lethality due to the lipopolysaccharide [3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途