阿拉普利

阿拉普利用途

阿拉西普利(Cetapril)是一种口服活性血管紧张素转换酶(ACE)抑制剂,具有持久的降压作用[1]。
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阿拉普利名称

[ CAS 号 ]:
74258-86-9

[ 中文名 ]:
阿拉普利

[ 英文名 ]:
Alacepril

[中文别名 ]:

[英文别名 ]:

阿拉普利生物活性

[ 描述 ]:

阿拉西普利(Cetapril)是一种口服活性血管紧张素转换酶(ACE)抑制剂,具有持久的降压作用[1]。

[ 相关类别 ]:

研究领域 >> 心血管疾病
信号通路 >> 代谢酶/蛋白酶 >> 血管紧张素转换酶(ACE)

[体内研究]

每日连续口服一次(1-2 mg/kg/d)可证实阿拉西普利对肾性高血压大鼠的长期降压作用。在肾性高血压犬中,阿拉西普利(3 mg/kg)表现出稳定和持续的降压作用,其作用时间长于卡托普利[1]。

[参考文献]

[1]. Takeyama K, et al. Antihypertensive activity of alacepril, an orally active angiotensin converting enzyme inhibitor, in renal hypertensive rats and dogs. Arzneimittelforschung. 1985;35(10):1502-1507.

阿拉普利物理化学性质

[ 密度 ]:
1.281g/cm3

[ 沸点 ]:
679.1ºC at 760 mmHg

[ 分子式 ]:
C20H26N2O5S

[ 分子量 ]:
406.49600

[ 闪点 ]:
364.5ºC

[ 精确质量 ]:
406.15600

[ PSA ]:
129.08000

[ LogP ]:
2.03410

[ 折射率 ]:
1.581

[ 储存条件 ]:
-20°C，干燥，密封

阿拉普利毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SQ7325700
CHEMICAL NAME :
L-Phenylalanine, N-(1-(3-(acetylthio)-2-methyl-1-oxopropyl)-L-prolyl)- , (S)-
CAS REGISTRY NUMBER :
74258-86-9
LAST UPDATED :
199612
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C20-H26-N2-O5-S
MOLECULAR WEIGHT :
406.54

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 :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7033,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1872 mg/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7033,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>3 gm/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7033,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7033,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
2921 mg/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7033,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>3 gm/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7033,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #7477
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>1600 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: -,64,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
54600 mg/kg/26W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - changes in sodium
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7097,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9 gm/kg/30D-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Blood - normocytic anemia Blood - other changes
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7041,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
18 gm/kg/30D-C
TOXIC EFFECTS :
Gastrointestinal - other changes Liver - other changes Related to Chronic Data - death
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7061,1985 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
26 gm/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,5711,1985
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阿拉普利安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22:Harmful if swallowed.

[ WGK德国 ]:
3

[ RTECS号 ]:
UO3516500

阿拉普利合成路线

详细合成路线

阿拉普利上下游产品

阿拉普利上游产品

阿拉普利下游产品

阿拉普利制备

1.0g化合物(I)溶于含有N-甲基吗啉的二氯甲烷中，加入0.57g化合物(Ⅱ)，反应1h，得化合物(Ⅲ)。2.5g化合物(Ⅲ)在三氟乙酸-苯甲醚中反应1h，得1.8g阿拉普利。

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