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培哚普利

培哚普利用途

Perindopril是长效血管紧张素转换酶(ACE)抑制剂。
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培哚普利名称

[ CAS 号 ]:
82834-16-0

[ 中文名 ]:
培哚普利

[ 英文名 ]:
Perindopril

[中文别名 ]:

[英文别名 ]:

培哚普利生物活性

[ 描述 ]:

Perindopril是长效血管紧张素转换酶(ACE)抑制剂。

[ 相关类别 ]:

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

[参考文献]

[1]. Vaclavik J, Perindopril in the treatment of hypertension and cardiovascular diseases: evolution continues with the orodispersible dosage form. Vnitr Lek. 2013 Apr;59(4):290-4.

[2]. Napalkov DA. Therapy with perindopril: organoprotection, not just the antihypertensive effect. Kardiologiia. 2012;52(12):80-3.


[相关活性小分子]

血管紧张素 (1-7) | 卡托普利 | 马来酸依那普利 | 培哚普利 | 赖诺普利二水合物 | Phosphoramidon Disodium | 群多普利 | 福辛普利钠 | 盐酸喹那普利 | 雷米普利 | 西拉普利 | 依那普利那二水 | 奥马曲拉 | Temocapril HCl | 血啡-7

培哚普利物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
537.4±45.0 °C at 760 mmHg

[ 熔点 ]:
100-101°C

[ 分子式 ]:
C19H32N2O5

[ 分子量 ]:
368.468

[ 闪点 ]:
278.8±28.7 °C

[ 精确质量 ]:
368.231110

[ PSA ]:
95.94000

[ LogP ]:
3.36

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±3.1 mmHg at 25°C

[ 折射率 ]:
1.512

[ 储存条件 ]:
-20°C Freezer

培哚普利毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
NL5999400
CHEMICAL NAME :
11H-Indole-2-carboxylic acid, octahydro-1-(2-((1-ethoxycarbonyl)butyl)amino)-1-oxop ropyl)-, (2S-(1(R*(R*)),2-alpha,3a-beta,7a-beta))-
CAS REGISTRY NUMBER :
82834-16-0
LAST UPDATED :
199612
DATA ITEMS CITED :
15
MOLECULAR FORMULA :
C19-H32-N2-O5
MOLECULAR WEIGHT :
368.53

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 :
>3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
323 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>2500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - respiratory depression
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: 22,1673,1994
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
679 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
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 :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>500 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
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: 22,1679,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4102 mg/kg/78W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - interstitial nephritis Kidney, Ureter, Bladder - changes in bladder weight
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
365 mg/kg/52W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Metabolism (Intermediary) - lipids including transport
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: 22,1689,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
273 mg/kg/91D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2184 mg/kg/26W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - interstitial nephritis Kidney, Ureter, Bladder - changes in bladder weight
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
4600 mg/kg/26W-I
TOXIC EFFECTS :
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: 22,1711,1994 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
192 mg/kg
SEX/DURATION :
female 6-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 22,1729,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
416 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) 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: 22,1729,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1010 mg/kg
SEX/DURATION :
male 80 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - other measures of fertility
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: 22,1729,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
104 mg/kg
SEX/DURATION :
female 17-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - other neonatal measures or effects Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,446,1992
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培哚普利安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S24/25

[ WGK德国 ]:
3

培哚普利合成路线

详细合成路线

培哚普利上下游产品

培哚普利上游产品

培哚普利下游产品

培哚普利制备

化合物(I)和化合物(Ⅱ)进行缩合，然后水解即可得到培垛普利。
化合物(Ⅰ)可由化合物(Ⅲ)出发，经酯化、还原、水解再酯化得到。
化合物(Ⅱ)可由化合物(Ⅳ)和化合物(Ⅶ)进行还原氨解反应得到，收率52%。(可参见Lane C F．Synthesis，1975，135～146)
化合物(Ⅱ)也可由化合物(Ⅷ)和化合物(Ⅸ)进行还原氨解反应得到，收率64.4%。 (可参见Yamada Sun-Ichi，et a1．Tetrahedron Lett，1976，13：997-1000)

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相关药品：

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：培哚普利

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥589.0/100mg ￥1189.0/250mg ￥1789.0/500mg ￥2689.0/500g

联系人：李先生

产品详情：Perindopril

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥720.9/100mg ￥4428.9/1g ￥1544.9/250mg ￥2574.9/500mg

联系人：阿拉丁

产品详情：培哚普利

公司名：上海创赛科技有限公司

区域：上海市嘉定区

价格：
￥713.0/100mg ￥2822.0/500mg ￥588.0/100mg ￥1176.0/250mg

联系人：夏言

产品详情：[Perfemiker]Perindopril,98%

公司名：盼得（上海）国际贸易有限公司

区域：上海市徐汇区

价格：
￥需询单/500g ￥需询单/1kg ￥需询单/25kg ￥需询单/200kg

联系人：叶经理

产品详情：培哚普利

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