| Name | Fenspiride hydrochloride |
| Description | Fenspiride hydrochloride (Decaspiride) , an oxazolidinone spiro compound, is a drug used in the therapy of certain respiratory diseases. It is approved for use in Russia for the therapy of chronic and acute inflammatory diseases of ENT organs and the respiratory tract (like sinusitis, tracheobronchitis, otitis, laryngitis, and rhinopharyngitis), and for maintenance therapy of asthma. |
| 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 9 mg/mL (30.32 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : 54 mg/mL (181.95 mM), Sonication is recommended.
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| Keywords | respiratory diseases | Phosphodiesterase (PDE) | PDE4 | PDE3 | orally active | non-steroidal | Inhibitor | inhibit | HistamineReceptor | Histamine Receptor | guinea-pigs | Fenspiride Hydrochloride | Fenspiride hydrochloride | Fenspiride | antiinflammatory | AdrenergicReceptor | Adrenergic Receptor |
| Inhibitors Related | Meclizine dihydrochloride | Lidocaine | Famotidine | Octopamine hydrochloride | Sodium butanoate | Theobromine | Apremilast | Icariin | Alginic acid | Trazodone hydrochloride | Doxofylline | Sildenafil citrate |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bitter Compound library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |