82989-25-1

• 常用中文名：他扎司特
• 常用英文名：Tazanolast
• CAS号：82989-25-1
• 分子式：C₁₃H₁₅N₅O₃
• 分子量：289.29000
• 相关类别： 研究领域 炎症/免疫
• 发布时间：2018-04-14 08:00:00
• 更新时间：2024-01-02 22:55:46
• Tazanolast 是选择性的肥大细胞稳定药物。

名称

• 中文名: 他扎司特
• 英文名: Tazanolast
• 中文别名: 丁基-3'-(1H-四唑-5-基)苯酰羧酸; 2-(3-(2H-四唑-5-基)苯基氨基)-2-氧代乙酸丁酯
• 英文别名: WP-833; TO-188; Tazalest; Tazanol

物化性质

• 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℃

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.

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

安全

• 海关编码: 2933990090

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%