- 生物活性
Tazanolast 是选择性的肥大细胞稳定药物。
- 体外研究
Tazanolast, an orally active mast-cell-stabilizing drug, which has been shown to suppress passive cutaneous anaphylaxis, Schultz-Dale reaction in isolated tracheal muscle, and experimental asthma without antagonistic actions upon histamine- and leukotriene-D4-induced contraction, IgE-mediated or compound 48/80-induced histamine release from mast cells and lung fragments, compound 48/80-induced Ca
2+
uptake into mast cells from extracellular medium, compound 48/80-induced translocation of protein kinase C from the cytosol to the membrane fraction of mast cells, and inositol trisphosphate production without directly inhibiting phospholipase C in mast cells.
- 体内研究
Tazanolast administered before ozone exposure at doses of 30, 100, or 300 mg/kg inhibits ozone-induced airway hyperresponsiveness in a dose-dependent manner. Tazanolast administered after ozone exposure does not inhibit the airway hyperresponsiveness. Tazanolast does not significantly change the cell distribution of bronchoalveolar lavage (BAL) cells at 2 h after the exposure. Tazanolast significantly inhibits ozone-induced airway hyperresponsiveness in guinea pigs.
- 化学性质
白色或带黄白色结晶或结晶性粉末，略臭，味苦。易溶于丙酮，较易溶于甲醇、乙醇或乙腈，难溶于乙醚，几不溶于水。急性毒性LD
50
雄、雌小鼠，雄、雌大鼠(mg/kg)：＞4000，＞4000，＞4000，＞4000口服；＞4000，＞4000，＞4000，＞4000皮下注射；1145，1191，1423，1528腹腔注射；1126，1121，1119，1277静脉注射。
- 用于支气管哮喘。
医药
在冰浴冷却下，于30min内将草酸单丁酯单酰氯加到5-(3-氨基苯基)四唑在吡啶中的溶液，可得他扎司特。
