Fenspiride HCl

For research use only.

Catalog No.S4090

Fenspiride HCl Chemical Structure

CAS No. 5053-08-7

Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.

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Biological Activity

Description Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.
Features Produces less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities.
Targets
PDE4 [1] PDE3 [1]
4.16(pIC50) 3.44(pIC50)
In vitro

Fenspiride induces potentiation of the effects of isoprenaline and sodium nitroprusside with logEC50 of 4.1 and 3.5, respectively, in human isolated bronchi. [1]

In vivo Fenspiride, an antiinflammatory drug with low anti-cyclooxygenase activity, administered orally at 60-200 mg/kg inhibits neutrophil migration into peritoneal and air pouches cavities as well as exudation into peritoneal cavities induced by endotoxin but not induced by carrageenin in the rat. Fenspiride (200 mg/kg) inhibits the release of tumour necrosis factor by stimulated macrophages in a dose-dependent manner in the rat. [2] Fenspiride (Topically applied) is found to inhibit the development of sclerotic lesions in myringotomized rats, whereas intraperitoneal injections are ineffective. [3] Fenspiride (60 mg/kg) significantly reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum (4.2 ng/mL vs. 2.3 ng/mL) and in the bronchoalveolar lavage fluid (55.7 ng/mL vs. 19.7 ng/mL) of guinea-pigs with endotoxemia. Fenspiride (60 mg/kg) also significantly reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages, defined as their enhanced release of arachidonic acid metabolites as compared to cells from untreated controls upon stimulation with N-formyl-methionyl-phenylalanine. Fenspiride (60 mg/kg) reduces the increased serum concentrations of extracellular type II phospholipase A2, the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide in guinea-pigs with endotoxemia. [4]

Protocol

Solubility (25°C)

In vitro Water 59 mg/mL (198.79 mM)
DMSO 9 mg/mL (30.32 mM)
Ethanol Insoluble

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Chemical Information

Molecular Weight 296.79
Formula

C15H20N2O2.HCl

CAS No. 5053-08-7
Storage powder
in solvent
Synonyms N/A
Smiles C1CN(CCC12CNC(=O)O2)CCC3=CC=CC=C3.Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID