洛度沙胺
- CAS号:53882-12-5
- 英文名:Lodoxamide
- 中文名:洛度沙胺
- CBNumber:CB21179062
- 分子式:C11H6ClN3O6
- 分子量:311.63
- MOL File:53882-12-5.mol
- 熔点 :212° (dec)
- 密度 :1.78±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMF: 3 mg/ml; DMSO: 5 mg/ml; PBS (pH 7.2): 2 mg/mL
- 形态 :A solid
- 酸度系数(pKa) :2.07±0.50(Predicted)
- 颜色 :Off-white to pink
- 稳定性 :Hygroscopic
洛度沙胺性质、用途与生产工艺
- 生物活性 Lodoxamide (U-42585E free acid) 是作为肥大细胞稳定剂的抗过敏化合物, 用于研究哮喘和过敏性结膜炎。
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体外研究
Lodoxamide inhibits compound 48/80-induced histamine release and ionophore-induced 45 Ca influx with associated histamine release in purified rat peritoneal mast cells. The chemotactic response of eosinophils to fMLP as well as to IL-5 is significant and dose-dependent inhibited by Lodoxamide. Lodoxamide is also able to strongly inhibit the release of eosinophil peroxidase after IgA-dependent activation and, to a lesser extent, the release of eosinophil cationic protein and eosinophil-derived neurotoxin.
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体内研究
Lodoxamide has been demonstrated to have cromolyn-like activity when studied in the rat peritoneal mast cell assay (PCA) model3 and in Ascaris antigen-sensitized rhesus monkeys. When given intravenously, orally, or intrabronchially by aerosol, lodoxamide significantly inhibits the increased respiratory frequency and decreased tidal volume induced by antigen challenge in Ascaris-sensitized. anesthetized rhesus monkeys. Addition of lodoxamide tromethamine to Euro-Collins or University of Wisconsin solution results in a marked decrease in lung reperfusion injury as demonstrated by increased oxygenation, decreased microvascular permeability, and increased compliance. Patients treated with lodoxamide tromethamine demonstrate an improvement in daytime breathing difficulty, cough, sputum production, and sleep.
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