product name Fenspiride HCl
Description: Fenspiride is a bronchodilator with potent anti-inflammatory properties, it inhibits phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi. Fenspiride is an oxazolidinone spiro compound used as a drug in the treatment of certain respiratory diseases.
References: Eur J Pharmacol. 1998 Jan 2;341(1):79-86; Eur J Pharmacol. 1993 Jul 6;238(1):47-52.
296.79
Formula
C15H20N2O2.HCl
CAS No.
5053-08-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 59 mg/mL (198.8 mM)
Water: <1 mg/mL
Ethanol: 9 mg/mL (30.3 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Fenspiride induces potentiation of the effects of isoprenaline and sodium nitroprusside with logEC50 of 4.1 and 3.5, respectively, in human isolated bronchi. Kinase Assay: Cell Assay: |
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| 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. Fenspiride (Topically applied) is found to inhibit the development of sclerotic lesions in myringotomized rats, whereas intraperitoneal injections are ineffective. 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. |
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| References | Eur J Pharmacol. 1998 Jan 2;341(1):79-86; Eur J Pharmacol. 1993 Jul 6;238(1):47-52. |
