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上海市上海市普陀区
产品名：奥西那林
纯度：90.0%
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586-06-1生产厂家

586-06-1

586-06-1结构式

常用中文名：奥西那林
常用英文名：orciprenaline
CAS号：586-06-1
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：2018-02-20 08:00:00
更新时间：2024-01-05 22:08:29
Metaproterenol (Orciprenaline) 是一种直接作用的拟交感神经药,是 β2-肾上腺素能受体 (β2AR) 激动剂,其 IC50 为 68 nM。Metaproterenol 还具有抗炎活性。

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中文名	奥西那林
英文名	Orciprenaline
中文别名	间羟异丙基肾上腺素 5-(1-羟基-2-异丙基氨基乙基)苯-1,3-二酚
英文别名	1-(3,5-Dihydroxyphenyl)-1-hydroxy-2-isopropylaminoethane 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol Benzyl alcohol, 3,5-dihydroxy-α-((isopropylamino)methyl)- orciprenaline 1,3-Benzenediol, 5-(1-hydroxy-2-((1-methylethyl)amino)ethyl)- 5-[1-Hydroxy-2-[(1-methylethyl)amino]ethyl]-1,3-benzenediol 1-(3,5-Dihydroxyphenyl)-2-isopropylaminoethanol Metaproterenol 3,5-Dihydroxy-a-[(isopropylamino)methyl]benzyl Alcohol 5-[1-Hydroxy-2-(isopropylamino)ethyl]-1,3-benzenediol 5-[1-Hydroxy-2-(isopropylamino)ethyl]benzene-1,3-diol EINECS 209-569-1 1,3-Benzenediol, 5-[1-hydroxy-2-[(1-methylethyl)amino]ethyl]-

描述	Metaproterenol (Orciprenaline) 是一种直接作用的拟交感神经药,是 β2-肾上腺素能受体 (β2AR) 激动剂,其 IC50 为 68 nM。Metaproterenol 还具有抗炎活性。
相关类别	研究领域 >> 内分泌
靶点	IC50: 68 nM (β2-adrenergic receptor)[1]
体外研究	Metaproterenol(10μM；74小时；THP-1细胞和骨髓巨噬细胞)治疗可增强β-arrestin2及其与高葡萄糖诱导的THP-1细胞和骨髓巨噬细胞中IκBα的相互作用[1]。Metaproterenol(10μM；74小时；THP-1细胞和骨髓巨噬细胞)治疗导致高葡萄糖诱导的THP-1细胞和骨髓巨噬细胞中NF-κB的下调[1]。蛋白质印迹分析[1]细胞系：THP-1细胞和骨髓巨噬细胞浓度：10μM孵育时间：74小时结果：β-arrestin2增强及其与IκBα的相互作用。RT-PCR[1]细胞系：THP-1细胞和骨髓巨噬细胞浓度：10μM孵育时间：74小时结果：导致NF-κB下调。
体内研究	用间蛋白肾治疗Zucker糖尿病性脂肪大鼠12周减弱单核细胞活化以及肾脏和心脏中的促炎和促纤维化反应。因此,间蛋白肾可能对糖尿病肾脏和心血管并发症具有保护作用[1]。
参考文献	[1]. Noh H, et al. Beta 2-adrenergic receptor agonists are novel regulators of macrophage activation in diabetic renal and cardiovascular complications. Kidney Int. 2017 Jul;92(1):101-113. [2]. Ibrahim FA, et al. Highly sensitive spectrofluorimetric method for rapid determination of orciprenaline in biological fluids and pharmaceuticals. Luminescence. 2019 Feb;34(1):77-83.

密度	1.2±0.1 g/cm3
沸点	417.5±40.0 °C at 760 mmHg
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	0.13
蒸汽压	0.0±1.0 mmHg at 25°C
折射率	1.579

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DO1800000

CHEMICAL NAME :: Benzyl alcohol, 3,5-dihydroxy-alpha-((isopropylamino)methyl)-

CAS REGISTRY NUMBER :: 586-06-1

LAST UPDATED :: 199709

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C11-H17-N-O3

MOLECULAR WEIGHT :: 211.29

WISWESSER LINE NOTATION :: QR CQ EYQ1MY

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 286 ug/kg

TOXIC EFFECTS :: Behavioral - tremor Cardiac - arrhythmias (including changes in conduction) Vascular - BP elevation not characterized in autonomic section

REFERENCE :: AJMSA9 American Journal of the Medical Sciences. (Slack Inc., 6900 Grove Rd., Thorofare, NJ 08086) New series: V.1- 1841- Volume(issue)/page/year: 291,168,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3370 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 8,353,1966

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 67200 ug/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 8,353,1966

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >8130 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 8,353,1966

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 240 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - sympathomimetic

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 31,33,1972

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 295 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4011258

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 86 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Cardiac - pulse rate increase, without fall in BP Skin and Appendages - hair

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 38,474,1976

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 125 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 8,353,1966

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 30 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 8,353,1966

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 3110 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 8,353,1966

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 81300 ug/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 8,353,1966 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 800 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

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

REFERENCE :: RDCNBM Reproduccion. (Madrid, Spain) V.1-7, 1974-83. Discontinued. Volume(issue)/page/year: 5,31,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5007 No. of Facilities: 35 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 476 (estimated) No. of Female Employees: 255 (estimated)