7683-59-2

7683-59-2结构式

常用中文名：异丙肾上腺素
常用英文名：Isoproterenol
CAS号：7683-59-2
分子式：C₁₁H₁₇NO₃
分子量：211.258
相关类别：原料药呼吸系统用药平喘药
发布时间：2018-06-02 08:00:00
更新时间：2024-01-02 18:13:31
异丙肾上腺素是一种非选择性的口服活性β-肾上腺素受体激动剂。异丙肾上腺素具有强大的外周血管扩张剂、支气管扩张剂和心脏刺激活性。异丙肾上腺素可用于研究心动过缓和支气管哮喘[1][2][3][4][5][6]。

中文名	异丙肾上腺素
英文名	isoprenaline
中文别名	4-[(2-异丙氨基-1-羟基)乙基]-1,2-苯二酚 (-)-N-异丙基-L-去甲肾上腺素异丙肾
英文别名	Isoproterenol N-isopropyl-2-(3,4-dihydroxyphenyl)-2-hydroxyethylamine asiprenol asmalar Respifral isoprel Aludrin (+/-)-isoproterenol A 21 Aludrine

描述	异丙肾上腺素是一种非选择性的口服活性β-肾上腺素受体激动剂。异丙肾上腺素具有强大的外周血管扩张剂、支气管扩张剂和心脏刺激活性。异丙肾上腺素可用于研究心动过缓和支气管哮喘[1][2][3][4][5][6]。
相关类别	研究领域 >> 心血管疾病研究领域 >> 内分泌信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
体外研究	异丙肾上腺素(300 nM,3分钟)使完整大鼠脂肪细胞中颗粒cGMP和西洛他胺抑制的低Km cAMP磷酸二酯酶(cAMP PDE)活性增加约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。在不存在腺苷的情况下,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]。异戊二烯(5 nM和10μM)可增加环腺苷酸水平,西洛他胺(10 mM)、环腺苷酸特异性PDE(PDE 4)抑制剂罗利普拉姆(10 mM)和环GMP提升剂(50 nM ANF或30 nM SNP加100 nM DMPPO)可增强这种作用[3]。异丙肾上腺素将Giα-2基因的转录活性提高到对照值的140%,而Gsα的基因特异性杂交保持不变[4]。异丙肾上腺素(20 nM)增加了总iK的振幅,并导致iK激活曲线中约10 mV的负偏移,无论是在300 nM尼索地平的存在下还是在300 nM尼索地平的存在下,以阻断L型Ca2+电流[5]。在兔分离的起搏器细胞中,异戊二烯(20 nM)使窦房结起搏器的自发起搏器率增加16%[5]。
体内研究	异戊二烯(口服,0.27-0.64μg/kg)在狗体内通过相对少量的反应被广泛代谢[6]。动物模型：狗[1]剂量：0.27-0.64μg/kg给药：口服结果：尿液中排泄量基本不变,尿液中只有三分之一的放射性以O-甲基代谢物的形式存在。显示血浆放射性几乎完全是共轭异丙肾上腺素,这种代谢物占尿液放射性的80%以上。当血浆浓度较高时,显示的心率恢复到基线值。

密度	1.2±0.1 g/cm3
沸点	417.5±40.0 °C at 760 mmHg
熔点	165 - 170ºC
分子式	C₁₁H₁₇NO₃
分子量	211.258
闪点	179.7±17.9 °C
精确质量	211.120850
PSA	72.72000
LogP	0.25
外观性状	白色结晶粉末
蒸汽压	0.0±1.0 mmHg at 25°C
折射率	1.579
储存条件	2-8 °C，密封，干燥

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DO1750000

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

CAS REGISTRY NUMBER :: 7683-59-2

BEILSTEIN REFERENCE NO. :: 2213857

LAST UPDATED :: 199707

DATA ITEMS CITED :: 37

MOLECULAR FORMULA :: C11-H17-N-O3

MOLECULAR WEIGHT :: 211.29

WISWESSER LINE NOTATION :: QR BQ DYQ1MY1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human

DOSE/DURATION :: 14 ug/kg

TOXIC EFFECTS :: Cardiac - pulse rate increase, without fall in BP Cardiac - change in rate

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 355 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 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 :: Cardiac - arrhythmias (including changes in conduction)

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 57 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 :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 850 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 - mouse

DOSE/DURATION :: 450 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 :: 440 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Sense Organs and Special Senses (Eye) - lacrimation Gastrointestinal - changes in structure or function of salivary glands

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 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 :: 83 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 :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Sense Organs and Special Senses (Eye) - lacrimation Gastrointestinal - changes in structure or function of salivary glands

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 70 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 250 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 :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 250 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 - guinea pig

DOSE/DURATION :: 270 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Sense Organs and Special Senses (Eye) - lacrimation Gastrointestinal - changes in structure or function of salivary glands

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 320 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Sense Organs and Special Senses (Eye) - lacrimation Gastrointestinal - changes in structure or function of salivary glands

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Amphibian - frog

DOSE/DURATION :: 80 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 320 mg/kg/6D-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TCLo - Lowest published toxic concentration

ROUTE OF EXPOSURE :: Inhalation

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 250 mg/m3/30M/30D-C

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands Endocrine - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg/30D-C

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands Endocrine - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 210 mg/kg

SEX/DURATION :: male 7 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 750 ug/kg

SEX/DURATION :: female 1-19 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 20 ug/kg

SEX/DURATION :: female 20 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 10 ug/kg

SEX/DURATION :: female 8 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 :: 3 ug/kg

SEX/DURATION :: female 8 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 - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 3 ug/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - body wall

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 3 ug/kg

SEX/DURATION :: female 8 day(s) after conception

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

TYPE OF TEST :: Unscheduled DNA synthesis

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Unscheduled DNA synthesis

TYPE OF TEST :: Mutation test systems - not otherwise specified

MUTATION DATA

TEST SYSTEM :: Rodent - rat

DOSE/DURATION :: 600 mg/kg/10D

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 125,722,1967 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84487 No. of Facilities: 116 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 927 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 84487 No. of Facilities: 107 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 9570 (estimated) No. of Female Employees: 8201 (estimated)

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