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    Fenspiride HCl
    Fenspiride HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0798
    CAS #: 5053-08-7Purity ≥98%

    Description: Fenspiride (NAT-333; JP-428; NDR-5998A; Decaspiride; Espiran; trade names Eurespal, Pneumorel), an oxazolidinone spiro compound acting as a α adrenergic and H1 histamine receptor antagonist, is a bronchodilator with potent anti-inflammatory properties. Iit inhibits phosphodiesterase 4/3 (PDE4/3) 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.

    Related CAS#: 5053-06-5 (free base); 5053-08-7 (HCl)

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    Molecular Weight (MW)296.79
    FormulaC15H20N2O2.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)
    Other info

    Chemical Name: 8-(2-Phenylethyl)-1-oxa-3,8-diazaspiro(4.5)decan-2-one hydrochloride

    InChi Key: FIKFLLIUPUVONI-UHFFFAOYSA-N

    InChi Code: InChI=1S/C15H20N2O2.ClH/c18-14-16-12-15(19-14)7-10-17(11-8-15)9-6-13-4-2-1-3-5-13;/h1-5H,6-12H2,(H,16,18);1H

    SMILES Code: O=C1OC2(CCN(CCC3=CC=CC=C3)CC2)CN1.[H]Cl

    Synonyms

    NAT333; NAT 333; JP 428; JP428; NDR-5998A; NDR 5998A; NAT-333; JP-428; NDR5998A; Decaspiride; Espiran; Fenspiride HCl; Fenspiride hydrochloride; Fluiden. trade names Eurespal, Pneumorel


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    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.

    In VivoFenspiride, 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. 
    Animal modelRats
    Formulation & Dosage60-200 mg/kg; oral
    References

    Eur J Pharmacol. 1998 Jan 2;341(1):79-86; Eur J Pharmacol. 1993 Jul 6;238(1):47-52.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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