73803-48-2

• 常用中文名：卓波酰胺
• 常用英文名：Tripamide
• CAS号：73803-48-2
• 分子式：C₁₆H₂₀ClN₃O₃S
• 分子量：369.86600
• 相关类别： 信号通路 跨膜转运 钾通道
• 发布时间：2018-02-09 08:00:00
• 更新时间：2024-01-31 18:50:12
• 三酰胺是一种口服活性磺酰胺衍生利尿剂降压药[1]。

名称

• 中文名: 卓波酰胺
• 英文名: 4-Chloro-N-((3aR,4S,7R,7aS)-hexahydro-1H-4,7-methanoisoindol-2(3H)-yl)-3-sulfamoylbenzamide
• 英文别名: Normonal; Tripamide; 4,7-Methano-2H-isoindole,benzamide deriv.; E 614; Toripamide; ADR 033

物化性质

• 密度: 1.51g/cm3
• 分子式: C₁₆H₂₀ClN₃O₃S
• 分子量: 369.86600
• 精确质量: 369.09100
• PSA: 100.88000
• LogP: 3.72000
• 折射率: 1.673
• 储存条件: 库房通风低温干燥

生物活性

• 描述: 三酰胺是一种口服活性磺酰胺衍生利尿剂降压药[1]。
• 相关类别:
  研究领域 >> 代谢疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 体外研究: 三酰胺(小于10μg/ml)不会改变膜电位和电阻,但会抑制3-5 mM TEA存在时由外向电流脉冲诱发的峰值[1]。在肠系膜动脉中,三酰胺抑制血管周围神经刺激诱发的e.j.ps振幅。然而,重复刺激产生的促进过程受三酰胺的影响较小[1]。
• 体内研究: 在口服25ml/kg生理盐水的大鼠中,三酰胺(0.6-160mg/kg)以剂量依赖性方式增加尿量以及钠和氯的排泄。仅当剂量为160 mg/kg时,大鼠的钾排泄量才会增加[2]。Tripamide具有抗高血压作用,在以10 mg/kg/天的剂量给自发性高血压大鼠4周期间,Tripamide的尿量和钠排泄量增加了一倍,而大鼠的钾排泄量增加了<50%[2]。
• 参考文献:

  [1]. H Asada, et al. Effects of N-(4-azo-endo-tricyclo[5.2.1.0.(2.6)]-decan-4-yl)-4-chloro-3-sulfamoylbenzamide (E614; tripamide) on vascular smooth muscles. Gen Pharmaco. 1982;13(3):215-23.

  [2]. Philip Hampel, et al. Azosemide is more potent than bumetanide and various other loop diuretics to inhibit the sodium-potassium-chloride-cotransporter human variants hNKCC1A and hNKCC1B. Sci Rep. 2018 Jun 29;8(1):9877.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : CV2338880 CHEMICAL NAME : Benzamide, 3-(aminosulfonyl)-4-chloro-N-(octahydro-4,7-methano-2 H-isoindol-2-yl)- (3a-alpha,4-alpha,7-alpha,7a-alpha)- CAS REGISTRY NUMBER : 73803-48-2 BEILSTEIN REFERENCE NO. : 1663663 LAST UPDATED : 199612 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C16-H20-Cl-N3-O3-S MOLECULAR WEIGHT : 369.90 WISWESSER LINE NOTATION : T C555 A ENTJ EMVR DG CSZW 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 : >8 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >4 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >2500 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >2500 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-15,1982 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 5 gm/kg SEX/DURATION : female 8-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : YKRYAH Yakubutsu Ryoho. Medicinal Treatment. (Tokyo, Japan) V.1-14, 1968-81. Suspended. Volume(issue)/page/year: 12,651,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 40 gm/kg SEX/DURATION : female 8-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death REFERENCE : YKRYAH Yakubutsu Ryoho. Medicinal Treatment. (Tokyo, Japan) V.1-14, 1968-81. Suspended. Volume(issue)/page/year: 12,651,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 5 gm/kg SEX/DURATION : female 8-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - physical REFERENCE : YKRYAH Yakubutsu Ryoho. Medicinal Treatment. (Tokyo, Japan) V.1-14, 1968-81. Suspended. Volume(issue)/page/year: 12,651,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 520 mg/kg SEX/DURATION : female 7-19 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : YKRYAH Yakubutsu Ryoho. Medicinal Treatment. (Tokyo, Japan) V.1-14, 1968-81. Suspended. Volume(issue)/page/year: 12,669,1979