硫酸奥西那林

硫酸奥西那林用途

Metaproterenol hemisulfate (Orciprenaline hemisulfate) 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 hemisulfate 还具有抗炎活性。

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硫酸奥西那林名称

[ CAS 号 ]:
5874-97-5

[ 中文名 ]:
硫酸奥西那林

[ 英文名 ]:
Orciprenaline sulfate

[中文别名 ]:

[英文别名 ]:

Orciprenaline sulfate

硫酸奥西那林生物活性

[ 描述 ]:

[ 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.

硫酸奥西那林物理化学性质

[ 密度 ]:
1.199g/cm3

[ 沸点 ]:
417.5ºC at 760mmHg

[ 熔点 ]:
202-203°

[ 分子式 ]:
C₁₁H₁₇NO_3.1/₂H₂O₄S

[ 分子量 ]:
520.59400

[ 闪点 ]:
179.7ºC

[ 精确质量 ]:
520.20900

[ PSA ]:
228.42000

[ LogP ]:
3.46820

[ 储存条件 ]:
-20°C，充氩

[ 水溶解性 ]:
Freely soluble in water, slightly soluble in ethanol (96 per cent), practically insoluble in methylene chloride.

硫酸奥西那林MSDS

详细MSDS(安全技术说明书)

硫酸奥西那林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DO2275000

CAS REGISTRY NUMBER :: 5874-97-5

LAST UPDATED :: 199606

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C22-H34-N2-O6.H2-O4-S

MOLECULAR WEIGHT :: 520.66

WISWESSER LINE NOTATION :: QR DQ BYQ1MY1&1 2 WSQQ

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 :: 5538 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: 18,185,1971

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 180,155,1969

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

ROUTE OF EXPOSURE :: Intraduodenal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2230 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 180,155,1969

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4800 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,521,1961

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 290 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,521,1961

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 114 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,521,1961 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 500 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 38,15,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5 gm/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) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 38,15,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 150 mg/kg

SEX/DURATION :: female 11-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 38,15,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3133 No. of Facilities: 1204 (estimated) No. of Industries: 1 No. of Occupations: 7 No. of Employees: 23118 (estimated) No. of Female Employees: 9688 (estimated)

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硫酸奥西那林安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H332

[ 警示性声明 ]:
P261

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
20

[ 安全声明 (欧洲) ]:
36

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

[ WGK德国 ]:
2

[ RTECS号 ]:
DO2275000

硫酸奥西那林文献

Lipophilicity of amine neurotransmitter precursors, metabolites and related drugs estimated on various TLC plates.

J. Chromatogr. Sci. 52(9) , 1095-103, (2014)

The retention behavior for a series of amine neurotransmitters, their precursors, metabolites and structurally related drugs has been investigated in reversed-phase thin-layer chromatography using RP-...

Stimulation by transforming growth factor-α of DNA synthesis and proliferation of adult rat hepatocytes in primary cultures: modulation by α- and β-adrenoceptor agonists. Kimura, M., et al.

J. Pharmacol. Exp. Ther. 29 , 171, (1999)

Examination of the effects of increasing Gs protein on beta2-adrenergic receptor, Gs, and adenylyl cyclase interactions.

Biochem. Pharmacol. 54 , 61-72, (1997)

We have examined the effect of increased Gs protein levels on the abilities of three different beta2-agonists to induce GTP shifts and stimulate adenylyl cyclase response in an effort to investigate t...

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