他扎司特

中文名称:

他扎司特

中文同义词:

他扎司特;丁基-3-(1H-四唑-5-基)苯酰羧酸;塔赞司特

英文名称:

TAZANOLAST

英文同义词:

butyl 2-oxo-2-[3-(2H-tetrazol-5-yl)anilino]acetate;Butyl 3-(1H-tetrazol-5-y1)oxanilate;Tazalest;Tazanol;TO-188;TAZANOLAST;N-[3-(1H-Tetrazol-5-yl)phenyl]oxamidic acid butyl ester;Oxo[[3-(1H-tetrazol-5-yl)phenyl]amino]acetic acid butyl ester

CAS号:

82989-25-1

分子式:

C13H15N5O3

分子量:

289.29

EINECS号:

相关类别:

科研试剂;呼吸系统用药;平喘药;药物;平喘药物

Mol文件:

82989-25-1.mol

密度 

1.343

储存条件 

Sealed in dry,2-8°C

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LD50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。

用途 

用于支气管哮喘。

生产方法 

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。