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醋丁洛尔

醋丁洛尔用途

醋丁洛尔是一种口服活性β1肾上腺素能受体(β1AR)拮抗剂。醋丁洛尔用于高血压、心绞痛和心律失常的研究[1][2][3]。

醋丁洛尔名称

[ CAS 号 ]:
37517-30-9

[ 中文名 ]:
醋丁洛尔

[ 英文名 ]:
acebutolol

[中文别名 ]:

醋丁酰心安

[英文别名 ]:

アセブトロール
EINECS 253-539-0
acebutolol
IL 17803A
MFCD00599435
Acecor

醋丁洛尔生物活性

[ 描述 ]:

醋丁洛尔是一种口服活性β1肾上腺素能受体(β1AR)拮抗剂。醋丁洛尔用于高血压、心绞痛和心律失常的研究[1][2][3]。

[ 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 adrenoceptor

[体内研究]

醋丁洛尔是一种β受体阻滞剂,用于治疗高血压和心律失常。大鼠单次静脉注射(10 mg/kg)醋丁洛尔后,血浆清除率为61.9 mL/min/kg,分布体积为9.6 L/kg,消除半衰期为1.8小时。大鼠单次静脉注射(50 mg/kg)醋丁洛尔后,血浆清除率为46.5 mL/min/kg,分布体积为9.5 L/kg,消除半衰期为2.3小时[1]。在Sprague-Dawley大鼠中,测得1分钟和10分钟后,乙酰丁洛尔(30 mg/kg)的心输出量分别减少65%和31%。与Sprague-Dawley大鼠的基线值相比,在测量1分钟或10分钟后,醋丁洛尔(30 mg/kg)显著减少大多数器官的局部血流量(RBF)[3]。

[参考文献]

[1]. Piquette-Miller, M. and F. Jamali, Pharmacokinetics and multiple peaking of acebutolol enantiomers in rats. Biopharm Drug Dispos, 1997. 18(6): p. 543-56.

[2]. Bristow MR, et al. Treatment of chronic heart failure with β-adrenergic receptor antagonists: a convergence of receptor pharmacology and clinical cardiology. Circ Res. 2011 Oct 28;109(10):1176-94.

[3]. Mostafavi, S., R. Lewanczuk, and R. Foster, Influence of acebutolol and metoprolol on cardiac output and regional blood flow in rats. Biopharm Drug Dispos, 2000. 21(4): p. 121-8.

醋丁洛尔物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
564.1±50.0 °C at 760 mmHg

[ 熔点 ]:
119-123ºC

[ 分子式 ]:
C₁₈H₂₈N₂O₄

[ 分子量 ]:
336.426

[ 闪点 ]:
295.0±30.1 °C

[ 精确质量 ]:
336.204895

[ PSA ]:
87.66000

[ LogP ]:
1.95

[ 外观性状 ]:
晶体

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.543

[ 储存条件 ]:
库房通风低温干燥

[ 水溶解性 ]:
259 mg/L

醋丁洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: EJ3500500

CHEMICAL NAME :: Butanamide, N-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)prop oxy)phenyl)-, (+-)-

CAS REGISTRY NUMBER :: 37517-30-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C18-H28-N2-O4

MOLECULAR WEIGHT :: 336.48

WISWESSER LINE NOTATION :: 3VMR CV1 DO1YQ1MY1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 152 mg/kg

TOXIC EFFECTS :: Cardiac - change in conduction velocity Vascular - BP lowering not characterized in autonomic section

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 20,69,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 137 mg/kg/24D-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 111,533,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 109 mg/kg/22D-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 111,533,1989

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 125 mg/kg

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

REFERENCE :: CKFRAY Ceskoslovenska Farmacie. (PNS-Ustredni Expedice a Dovoz Tisku, Kafkova 19, 160 00 Prague 6, Czechoslovakia) V.1- 1952- Volume(issue)/page/year: 42,82,1993

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 75200 ug/kg

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

REFERENCE :: NPMDAD Nouvelle Presse Medicale. (Paris, France) V.1-11, 1972-82. Volume(issue)/page/year: 7,3258,1978

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 4 mg/kg

TOXIC EFFECTS :: Cardiac - change in rate Vascular - BP lowering not characterized in autonomic section Kidney, Ureter, Bladder - changes in blood vessels or in circulation of kidney

REFERENCE :: MASODV Masui to Sosei. Anesthesia and Resuscitation. (Hiroshima Masui Igakkai, Hiroshima Daigaku Igakubu Masuigaku Kyoshitsu, 1-2-3 Kasumi, Minami-ku, Hiroshima, Hiroshima, Japan) V.6- 1970- Volume(issue)/page/year: 16,13,1980 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 120 mg/kg

SEX/DURATION :: female 34-39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - respiratory system

REFERENCE :: DPTHDL Developmental Pharmacology and Therapeutics. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 4(Suppl 1),109,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 1080 mg/kg

SEX/DURATION :: female 1-39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - biochemical and metabolic

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 283,1077,1981

醋丁洛尔安全信息

[ 海关编码 ]:
2924299090

醋丁洛尔制备

【方法一】
由5'-丁酰胺-2'-(2,3-环氧丙氧)乙酰苯、异丙胺反应制得。

醋丁洛尔海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%