盐酸芬司必利
货号：
IF1210
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| MDL | MFCD00133315 |
| EC | EINECS 225-752-9 |
| 别名 | 芬司匹利盐酸盐 |
| 英文名称 | Fenspiride Hydrochloride |
| CAS | 5053-08-7 |
| 分子式 | C15H20N2O2·HCl |
| 分子量 | 296.79 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | White to pale yellow Powder |
| 单位 | 瓶 |
| 生物活性 | Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1-3]. |
| In Vitro | Fenspiride (around 100 μM) inhibits histamine-induced contraction of isolated guinea pig trachea.Fenspiride (≤1000 μM) produces less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities[2]. |
| In Vivo | Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum and in the bronchoalveolar lavage fluid (BALF) of the model of endotoxemia.Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages.Fenspiride (60 mg/kg; p.o. for 3 days) reduces the increased serum concentrations of extracellular type II phospholipase A 2, the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide[3]. |
| SMILES | O=C1OC2(CCN(CCC3=CC=CC=C3)CC2)CN1.[H]Cl |
| 靶点 | Adrenergic Receptor，Histamine Receptor，PDE |
| 数据来源文献 | [1]. Matuszewska A, et al. Long-term administration of fenspiride has no negative impact on bone mineral density and bone turnover in young growing rats. Adv Clin Exp Med. 2019 Jun;28(6):771-776. [2]. Cortijo J, et al. Effects of fenspiride on human bronchial cyclic nucleotide phosphodiesterase isoenzymes: functional and biochemical study. Eur J Pharmacol. 1998 Jan 2;341(1):79-86. [3]. De Castro CM, et al. Fenspiride: an anti-inflammatory drug with potential benefits in the treatment of endotoxemia. Eur J Pharmacol. 1995 Dec 29;294(2-3):669-76. |
| 规格 | 50mg 100mg 200mg |
是肾上腺素能受体和H1受体拮抗剂。