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卓波酰胺

卓波酰胺用途

三酰胺是一种口服活性磺酰胺衍生利尿剂降压药[1]。
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卓波酰胺名称

[ CAS 号 ]:
73803-48-2

[ 中文名 ]:
卓波酰胺

[ 英文名 ]:
Tripamide

[英文别名 ]:

卓波酰胺生物活性

[ 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.

卓波酰胺物理化学性质

[ 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

卓波酰胺毒性和生态

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
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区域：上海市普陀区

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产品详情：Tripamide

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