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Fenspiride hydrochloride

CAS No. : 5053-08-7

MCE 国际站：Fenspiride hydrochloride

产品活性：Fenspiride 是一种口服活性的非甾体抗炎剂，是 H1-组胺受体 (H1-histamine receptors) 的拮抗剂。Fenspiride 抑制磷酸二酯酶 3 (PDE3)、磷酸二酯酶 4 (PDE4)和磷酸二酯酶 5 (PDE5) 的活性，-log IC₅₀ 值分别为 3.44、4.16 和大约 3.8。Fenspiride 可用于呼吸系统疾病的研究。

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

作用靶点：Histamine Receptor  |  Phosphodiesterase (PDE)

In Vitro: Fenspiride (around 100 μM) inhibits histamine-induced contraction of isolated guinea pig trachea.
Fenspiride (≤1000 μM) produces less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities.

In Vivo: Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum and in the bronchoalveolar lavage fluid (BALF) of the model of endotoxemia.
Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages.
Fenspiride (60 mg/kg; p.o. for 3 days) reduces 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.

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