洛度沙胺
洛度沙胺 性质
| 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：3mg/mL； DMSO：5mg/mL； PBS（pH 7.2）：2 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 2.07±0.50(Predicted) |
| 颜色 | 米白色至粉红色 |
| 稳定性 | 吸湿性 |
| InChI | 1S/C11H6ClN3O6/c12-7-5(14-8(16)10(18)19)1-4(3-13)2-6(7)15-9(17)11(20)21/h1-2H,(H,14,16)(H,15,17)(H,18,19)(H,20,21) |
| InChIKey | RVGLGHVJXCETIO-UHFFFAOYSA-N |
| SMILES | Clc1c(cc(cc1NC(=O)C(=O)O)C#N)NC(=O)C(=O)O |
洛度沙胺 用途与合成方法
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.
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.
