盐酸塞利洛尔

盐酸塞利洛尔用途

Celiprolol hydrochloride 是一种有效的、选择性和具有口服活性的 β1 肾上腺素受体拮抗剂,具有部分 β2 激动剂活性,因此它是一种选择性肾上腺素受体调节剂 (SAM)。Celiprolol hydrochloride 具有降压和抗心绞痛的活性。

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盐酸塞利洛尔名称

[ CAS 号 ]:
57470-78-7

[ 中文名 ]:
盐酸塞利洛尔

[ 英文名 ]:
Celiprolol HCl

[中文别名 ]:

[英文别名 ]:

MFCD00941500
Celiprolol Hydrochloride
UNII:G1M3398594
EINECS 260-752-2
Celiprolol HCl

盐酸塞利洛尔生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[ 靶点 ]

β1-andrenoceptor[1]

[体内研究]

西利普洛尔(5或50 mg/kg；每天p.o.连续12周)在50 mg/kg剂量下具有中度降压作用,并显著减轻SHR肠系膜动脉中层平滑肌肥大[2]。动物模型：雄性自发性高血压大鼠(SHR)和同龄Wistar-Kyoto(WKY)大鼠(8周龄)[2]剂量：5,50mg/kg给药：P.o.每天(饮用水中给药),持续12周。结果：50mg/kg剂量组SHR血压升高明显减轻。对心脏或体重没有显著影响。SHR肠系膜动脉平均中层厚度减小。

[参考文献]

[1]. Nawarskas JJ, et, al. Celiprolol: A Unique Selective Adrenoceptor Modulator. Cardiol Rev. Sep/Oct 2017; 25(5): 247-253.

[2]. Tolvanen JP, et, al. Effect of celiprolol therapy on arterial dilatation in experimental hypertension. Br J Pharmacol. 1996 Nov; 119(6): 1137-44.

盐酸塞利洛尔物理化学性质

[ 密度 ]:
1.114g/cm3

[ 沸点 ]:
586.5ºC at 760 mmHg

[ 熔点 ]:
197-200ºC (dec.)

[ 分子式 ]:
C₂₀H₃₄ClN₃O₄

[ 分子量 ]:
415.955

[ 闪点 ]:
308.5ºC

[ 精确质量 ]:
415.223785

[ PSA ]:
94.39000

[ LogP ]:
4.09720

[ 外观性状 ]:
白色结晶固体

[ 储存条件 ]:
Refrigerator

盐酸塞利洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YR6560000

CHEMICAL NAME :: Urea, 3-(3-acetyl-4-(3-((1,1-dimethylethyl)amino)-2-hydroxy propoxy)phenyl)-1,1-d iethyl-, monohydrochloride

CAS REGISTRY NUMBER :: 57470-78-7

LAST UPDATED :: 199709

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C20-H33-N3-O4.Cl-H

MOLECULAR WEIGHT :: 416.02

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 40 mg/kg/2W-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 26,842,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2157 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 754 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 68300 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,41,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1362 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 310 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 42300 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 512 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - nausea or vomiting

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,41,1983

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盐酸塞利洛尔文献

Highly sensitive transient isotachophoresis sample stacking coupling with capillary electrophoresis-amperometric detection for analysis of doping substances

Talanta 81(4-5) , 1288-94, (2010)

A simple and effective method of capillary electrophoresis-amperometric detection (CE–AD) coupled with transient isotachophoresis (tITP) was developed for the trace determination of doping substances....

Simultaneous separation of eight beta-adrenergic drugs using titanium dioxide nanoparticles as additive in capillary electrophoresis.

Electrophoresis 29(11) , 2321-9, (2008)

The analysis is described for separating seven beta-adrenergic blocking agents (atenolol, celiprolol, clorprenaline, fenoterol, metoprolol, propranolol, terbutaline) and clenbuterol (sympathomimetic b...

Direct determination of celiprolol in human urine using on-line coupled ITP-CZE method with fiber-based DAD.

Electrophoresis 29(22) , 4561-7, (2008)

The present work illustrated possibilities of column-coupling electrophoresis combined with DAD for the direct quantitative determination of trace drug (celiprolol, CEL) in clinical human urine sample...

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