| CAS NO: | 5053-08-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| 25g | 电议 |
| 50g | 电议 |
| Molecular Weight (MW) | 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) | |
| 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 |
| 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 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. |
| Animal model | Rats |
| Formulation & Dosage | 60-200 mg/kg; oral |
| References | Eur J Pharmacol. 1998 Jan 2;341(1):79-86; Eur J Pharmacol. 1993 Jul 6;238(1):47-52. |
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