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盐酸异丙肾上腺素

盐酸异丙肾上腺素用途

Isoprenaline hydrochloride是一种非选择性的β-肾上腺素能受体激动剂,具有有效的外周血管扩张剂,支气管扩张剂和心脏刺激活性。

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盐酸异丙肾上腺素名称

[ CAS 号 ]:
51-30-9

[ 中文名 ]:
盐酸异丙肾上腺素

[ 英文名 ]:
Isoprenaline hydrochloride

[中文别名 ]:

异丙肾上腺素盐酸盐

[英文别名 ]:

Isoproterenol hydrochloride
Mistarel
Isovon
euspiran
Isoprenaline HCl
EINECS 200-089-8
Saventrine IV
(±)-Isoproterenol hydrochloride
Suscardia
isoprenaline

盐酸异丙肾上腺素生物活性

[ 描述 ]:

Isoprenaline hydrochloride是一种非选择性的β-肾上腺素能受体激动剂,具有有效的外周血管扩张剂,支气管扩张剂和心脏刺激活性。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 心血管疾病

[ 靶点 ]

Beta-adrenergic receptor[1]

[体外研究]

异丙肾上腺素(300 nM,3 min)在完整大鼠脂肪细胞中增加颗粒cGMP-和西洛他敏抑制的低Km cAMP磷酸二酯酶(cAMP-PDE)活性约100％[1]。异丙肾上腺素抑制大鼠脂肪细胞中胰岛素刺激的葡萄糖转运活性。在没有腺苷的情况下,异丙肾上腺素促进胰岛素刺激的细胞表面GLUT4的可及性的时间依赖性(t1/2约2分钟)降低> 50％,这与观察到的转运活性抑制直接相关[2]。。异丙肾上腺素(5 nM和10 mM)增加环磷酸腺苷水平,这种作用可被西洛他胺(10 mM),环丙沙坦,环AMP特异性PDE(PDE 4)抑制剂(10 mM)和环GMP升高剂( 50 nM ANF或30 nM SNP加100 nM DMPPO)[3]。异丙肾上腺素使Giα-2基因的转录活性增加至对照值的140％,而Gsα的基因特异性杂交保持不变[4]。异丙肾上腺素(20nM)增加总iK的幅度并在iK的激活曲线中引起约10mV的负偏移,在不存在和存在300nM尼索地平的情况下阻断L型Ca2 +电流。在兔离体起搏细胞中,异丙肾上腺素(20 nM)使窦房结起搏细胞的自发起搏器率增加16％[5]。

[细胞实验]

将细胞以每孔2至5×10 4个细胞的密度接种在24孔培养皿中。当细胞达到汇合时，在培养3至5天后进行实验。吸出培养基并用0.5mL含有药理学试剂的PBS代替。处理在37℃下一式四份进行。分别将3,4和5型PDE抑制剂西洛酰胺（10gM），咯利普兰（10pM）和DMPPO（10gM）与细胞一起温育30分钟，然后加入腺苷酸或鸟苷酸环化酶激活剂。通过用ANF（50nM，10分钟）刺激颗粒状鸟苷酸环化酶或使用异丙肾上腺素（5nm，5分钟）的fl-肾上腺素能受体，在RASMC中分别增加环状GMP和环AMP。在孵育期结束时，除去培养基并通过两次乙醇（65％）洗涤在4℃下提取细胞内环核苷酸5分钟。合并乙醇提取物，通过Speed-Vac系统蒸发至干燥。将干燥的提取物溶解在适量的测定缓冲液中，并通过闪烁亲近测定法测量环核苷酸水平。

[参考文献]

[1]. Degerman E, et al. Evidence that insulin and isoprenaline activate the cGMP-inhibited low-K_m cAMP phosphodiesterase in rat fat cells by phosphorylation. Proc Natl Acad Sci U S A. 1990 Jan;87(2):533-7

[2]. Vannucci SJ, et al. Cell surface accessibility of GLUT4 glucose transporters in insulin-stimulated rat adipose cells. Modulation by isoprenaline and adenosine. Biochem J. 1992 Nov 15;288 (Pt 1):325-30.

[3]. Delpy E, et al. Effects of cyclic GMP elevation on isoprenaline-induced increase in cyclic AMP and relaxation in rat aortic smooth muscle: role of phosphodiesterase 3. Br J Pharmacol. 1996 Oct;119(3):471-8.

[4]. Muller FU, et al. Isoprenaline stimulates gene transcription of the inhibitory G protein alpha-subunit Gi alpha-2 in rat heart. Circ Res. 1993 Mar;72(3):696-700.

[5]. Lei M, et al. Modulation of delayed rectifier potassium current, iK, by isoprenaline in rabbit isolated pacemaker cells. Exp Physiol. 2000 Jan;85(1):27-35.

[相关活性小分子]

盐酸异丙肾上腺素物理化学性质

[ 密度 ]:
1.324 g/cm3

[ 沸点 ]:
417.5ºC at 760 mmHg

[ 熔点 ]:
165-175 °C (dec.)(lit.)

[ 分子式 ]:
C₁₁H₁₈ClNO₃

[ 分子量 ]:
247.719

[ 闪点 ]:
179.7ºC

[ 精确质量 ]:
247.097519

[ PSA ]:
72.72000

[ LogP ]:
2.32210

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
Store at RT

[ 稳定性 ]:
Stable, but may be air and light sensitive. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
Soluble

盐酸异丙肾上腺素MSDS

详细MSDS(安全技术说明书)

盐酸异丙肾上腺素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DO1925000

CHEMICAL NAME :: Benzyl alcohol, 3,4-dihydroxy-alpha-((isopropylamino)methyl)-, hydrochloride

CAS REGISTRY NUMBER :: 51-30-9

LAST UPDATED :: 199707

DATA ITEMS CITED :: 23

MOLECULAR FORMULA :: C11-H17-N-O3.Cl-H

MOLECULAR WEIGHT :: 247.75

WISWESSER LINE NOTATION :: QR BQ DYQ1MY1&1 &GH

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 :: 2221 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 128 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 600 ug/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 26900 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1260 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 450 mg/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 60 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 77 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 600 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 50 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 3070 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 27 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 930 mg/kg/31D-I

TOXIC EFFECTS :: Cardiac - other changes Cardiac - changes in heart weight Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg/30D-I

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands Endocrine - changes in adrenal weight Endocrine - changes in spleen weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 10 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 5 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2500 ug/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 13 mg/L

REFERENCE :: EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987- Volume(issue)/page/year: 10(Suppl 10),1,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 82898 No. of Facilities: 1655 (estimated) No. of Industries: 3 No. of Occupations: 10 No. of Employees: 6062 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 82898 No. of Facilities: 649 (estimated) No. of Industries: 3 No. of Occupations: 8 No. of Employees: 18945 (estimated) No. of Female Employees: 8469 (estimated)

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盐酸异丙肾上腺素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi:Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
DO1925000

盐酸异丙肾上腺素合成路线

详细合成路线

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盐酸异丙肾上腺素制备

同邻苯二酚为原料制得

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盐酸异丙肾上腺素文献

Developing structure-activity relationships for the prediction of hepatotoxicity.

Chem. Res. Toxicol. 23 , 1215-22, (2010)

Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals ...

A predictive ligand-based Bayesian model for human drug-induced liver injury.

Drug Metab. Dispos. 38 , 2302-8, (2010)

Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

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盐酸异丙肾上腺素

盐酸异丙肾上腺素用途

盐酸异丙肾上腺素名称

盐酸异丙肾上腺素生物活性

盐酸异丙肾上腺素物理化学性质

盐酸异丙肾上腺素MSDS

详细MSDS(安全技术说明书)

盐酸异丙肾上腺素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

盐酸异丙肾上腺素安全信息

盐酸异丙肾上腺素合成路线

详细合成路线

盐酸异丙肾上腺素上下游产品

盐酸异丙肾上腺素上游产品

盐酸异丙肾上腺素下游产品

盐酸异丙肾上腺素制备

盐酸异丙肾上腺素文献

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