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82989-25-1

中文名稱 他扎司特
英文名稱 TAZANOLAST
CAS 82989-25-1
分子式 C13H15N5O3
分子量 289.29
MOL 文件 82989-25-1.mol
82989-25-1 結(jié)構(gòu)式 82989-25-1 結(jié)構(gòu)式

基本信息

中文別名
塔贊司特
他扎司特
化合物 T17001
丁基-3'-(1H-四唑-5-基)苯酰羧酸
英文別名
WP-833
TO-188
Tazanol
Tazalest
TAZANOLAST
Tazanolast(Tazalest,TO 188,WP 833)
Butyl 3'-(1H-tetrazol-5-y1)oxanilate
butyl 2-oxo-2-[3-(2H-tetrazol-5-yl)anilino]acetate
N-[3-(1H-Tetrazol-5-yl)phenyl]oxamidic acid butyl ester
Butyl 2-((3-(1H-tetrazol-5-yl)phenyl)aMino)-2-oxoacetate
所屬類別
藥物: 呼吸系統(tǒng)用藥: 平喘藥

物理化學(xué)性質(zhì)

外觀性狀白色或帶黃白色結(jié)晶或結(jié)晶性粉末,略臭,味苦。易溶于丙酮,較易溶于甲醇、乙醇或乙腈,難溶于乙醚,幾不溶于水。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靜脈注射。
密度1.343
儲存條件2-8°C
溶解度Soluble in DMSO
酸度系數(shù)(pKa)4.06±0.10(Predicted)
形態(tài)Solid
顏色White to off-white

應(yīng)用領(lǐng)域

用途1
用于支氣管哮喘。

制備方法

方法1
在冰浴冷卻下,于30min內(nèi)將草酸單丁酯單酰氯加到5-(3-氨基苯基)四唑在吡啶中的溶液,可得他扎司特。

上下游產(chǎn)品信息

常見問題列表

生物活性
Tazanolast 是選擇性的肥大細(xì)胞穩(wěn)定藥物。
體外研究

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.

體內(nèi)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.

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