西罗普利

西罗普利用途

Ceronapril(SQ 29852)是一种有效的口服活性血管紧张素转换酶(ACE)抑制剂,IC50为36 nM[1]。

西罗普利名称

[ CAS 号 ]:
111223-26-8

[ 中文名 ]:
西罗普利

[ 英文名 ]:
Ceronapril

[英文别名 ]:

Ceranapril
CERONAPRIL
SQ-29,852
Ceronaprilum

西罗普利生物活性

[ 描述 ]:

Ceronapril(SQ 29852)是一种有效的口服活性血管紧张素转换酶(ACE)抑制剂,IC50为36 nM[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)

[ 靶点 ]

IC50: 36 nM (ACE)[1]

[体内研究]

塞罗那普利(SQ 29852)在雄性标准差大鼠中抑制王牌静脉注射和口服的第50版分别为 0.063μM/kg和 0.53μ塞罗那普利(100 mg/kg；口服；单剂量或每日两次,持续3天)阻断大鼠外周部位的王牌[2]动物模型：雄性Sprague-Dawley大鼠[2]剂量：100 mg/kg给药：PO,每天两次,连续3天或每天一次。单次给药后迅速(3小时)抑制血浆、肾脏和肺中的ACE。未抑制血脑屏障内大脑结构中的ACE,如尾壳核、脉络丛、苍白球、视上核和下丘脑脑室旁核。

[参考文献]

[1]. Karanewsky D S, et al. (Phosphinyloxy) acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy (4-phenylbutyl) phosphinyl] oxy]-1-oxohexyl]-L-proline, a novel orally active inhibitor of ACE. Journal of medicinal chemistry, 1988, 31(1): 204-212.

[2]. Chen BZ, et al. Effect of acute and chronic administration of ceronapril on angiotensin converting enzyme in plasma, kidney, lung, brain regions and cerebrospinal fluid of rats. Neuropharmacology. 1992 Sep;31(9):929-35.

西罗普利物理化学性质

[ 密度 ]:
1.265g/cm3

[ 沸点 ]:
682.8ºC at 760 mmHg

[ 分子式 ]:
C₂₁H₃₃N₂O₆P

[ 分子量 ]:
440.47000

[ 闪点 ]:
366.7ºC

[ 精确质量 ]:
440.20800

[ PSA ]:
139.97000

[ LogP ]:
3.42270

[ 蒸汽压 ]:
1.4E-19mmHg at 25°C

[ 折射率 ]:
1.559

西罗普利毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TW3589050

CHEMICAL NAME :: L-Proline, 1-(6-amino-2-((hydroxy(4-phenylbutyl)phosphinyl)oxy)- 1-oxohexyl)-, (S)-

CAS REGISTRY NUMBER :: 111223-26-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C21-H33-N2-O6-P

MOLECULAR WEIGHT :: 440.53

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 :: >5 gm/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - 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: 20,3875,1992

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2500 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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: 20,3875,1992

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,379,1992 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 720 mg/kg

SEX/DURATION :: female 6-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

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: 22,3401,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 31 gm/kg

SEX/DURATION :: female 15-45 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

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: 22,3401,1994