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他扎司特

他扎司特用途

Tazanolast 是选择性的肥大细胞稳定药物。
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他扎司特名称

[ CAS 号 ]:
82989-25-1

[ 中文名 ]:
他扎司特

[ 英文名 ]:
Tazanolast

[中文别名 ]:

[英文别名 ]:

他扎司特生物活性

[ 描述 ]:

Tazanolast 是选择性的肥大细胞稳定药物。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他
研究领域 >> 炎症/免疫

[体外研究]

Tazanolast,一种口服活性肥大细胞稳定药物,已被证明可抑制被动皮肤过敏反应,孤立气管肌中的Schultz-Dale反应,以及对组胺和白三烯-D4诱导的收缩无拮抗作用的实验性哮喘,IgE-介导或化合物48/80诱导肥大细胞和肺片段释放组胺,化合物48/80诱导Ca2 +从细胞外培养基中摄入肥大细胞,化合物48/80诱导蛋白激酶C从细胞质转运至膜组分肥大细胞和肌醇三磷酸的产生,不直接抑制肥大细胞中的磷脂酶[1]。

[体内研究]

在臭氧暴露之前以30,100或300mg/kg的剂量施用的Tazanolast以剂量依赖性方式抑制臭氧诱导的气道高反应性。臭氧暴露后施用的Tazanolast不会抑制气道高反应性。 Tazanolast在暴露后2小时不显着改变支气管肺泡灌洗(BAL)细胞的细胞分布。 Tazanolast显着抑制臭氧诱导的豚鼠气道高反应性[1]。

[动物实验]

猪[1] 10只豚鼠也暴露于2 ppm臭氧2小时，然后口服300 mg / kg Tazanolast（T-300 post group）。在暴露后2小时，测定每只动物的PC200-MCh。此后，对每只动物进行BAL。在第1天，测定50只豚鼠的暴露前PC200-MCh。在第2天，以10只为一组的豚鼠以30mg / kg（T-30组），100mg / kg（T-100组）或300mg / kg（T-300组）的剂量口服给予Tazanolast。 ），或单独的车辆（车辆组）。 30分钟后，将动物暴露于2ppm臭氧中2小时。此外，其他10只豚鼠也暴露于2ppm臭氧2小时，然后口服施用300mg / kg Tazanolast（T-300组）。在暴露后2小时，测定每只动物的PC200-MCh。此后，对每只动物进行BAL。

[参考文献]

[1]. Igarashi A, et al. Tazanolast inhibits ozone-induced airway hyperresponsiveness in guinea pigs. Am J Respir Crit Care Med. 1998 May;157(5 Pt 1):1531-5.


[相关活性小分子]

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他扎司特物理化学性质

[ 密度 ]:
1.343g/cm3

[ 分子式 ]:
C13H15N5O3

[ 分子量 ]:
289.29000

[ 精确质量 ]:
289.11700

[ PSA ]:
109.86000

[ LogP ]:
1.22150

[ 折射率 ]:
1.604

[ 储存条件 ]:
2-8℃

他扎司特毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AJ1480000
CHEMICAL NAME :
Acetic acid, oxo((3-(1H-tetrazol-5-yl)phenyl)amino)-, butyl ester
CAS REGISTRY NUMBER :
82989-25-1
LAST UPDATED :
199612
DATA ITEMS CITED :
14
MOLECULAR FORMULA :
C13-H15-N5-O3
MOLECULAR WEIGHT :
289.33

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1423 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - hypermotility, diarrhea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1119 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1120 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4778816
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1121 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - other changes
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,11,1989 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
57600 mg/kg/13W-I
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Blood - changes in bone marrow (not otherwise specified) Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,53,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
14840 mg/kg/53W-I
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,177,1989 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
24 gm/kg
SEX/DURATION :
female 13 day(s) pre-mating - 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,255,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
13200 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - delayed effects
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,265,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
30 gm/kg
SEX/DURATION :
female 17-20 day(s) after conception lactating female 22 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,283,1989
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他扎司特安全信息

[ 海关编码 ]:
2933990090

他扎司特海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

推荐生产厂家/供应商：

公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：Tazanolast

公司名：上海创赛科技有限公司

区域：上海市嘉定区

价格：
￥4752.0/1mg ￥9504.0/5mg

联系人：夏言

产品详情：[Perfemiker]Tazanolast,≥99%

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