奥西那林

生物活性靶点体外研究体内研究

奥西那林

CAS号:586-06-1
英文名:Orciprenaline
中文名:奥西那林
CBNumber:CB1855195
分子式:C11H17NO3
分子量:211.26
MOL File:586-06-1.mol

奥西那林化学性质

熔点 :100°
沸点 :350.94°C (rough estimate)
密度 :1.1240 (rough estimate)
折射率 :1.5718 (estimate)
酸度系数(pKa) :9.11±0.10(Predicted)
CAS 数据库 :586-06-1(CAS DataBase Reference)

奥西那林性质、用途与生产工艺

生物活性 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。
靶点

IC50: 68 nM (β2-adrenergic receptor)

体外研究

Metaproterenol (10 μM; 74 hours; THP-1 cells and bone marrow macrophages) treatment enhances β-arrestin2 and its interaction with IκBα in high glucose-induced THP-1 cells and bone marrow macrophages.
Metaproterenol (10 μM; 74 hours; THP-1 cells and bone marrow macrophages) treatment leads to downregulation of NF-κB in high glucose-induced THP-1 cells and bone marrow macrophages.

Western Blot Analysis

Cell Line:	THP-1 cells and bone marrow macrophages
Concentration:	10 μM
Incubation Time:	74 hours
Result:	Enhanced β-arrestin2 and its interaction with IκBα.

RT-PCR

Cell Line:	THP-1 cells and bone marrow macrophages
Concentration:	10 μM
Incubation Time:	74 hours
Result:	Led to downregulation of NF-κB.

体内研究

Treatment of Zucker diabetic fatty rats with Metaproterenol for 12 weeks attenuates monocyte activation as well as pro-inflammatory and pro-fibrotic responses in the kidneys and heart. Thus, Metaproterenol might has protective effects against diabetic renal and cardiovascular complications.
化学性质熔点100℃。其硫酸（[5874-97-5]）熔点202-203℃。
用途支气管扩张药。
生产方法 3，5-二乙酸基乙酰首先与溴反应，然后与异丙胺反应得过且过-（3，5-二羟基苯基）-2-异丙胺乙酮，将其溶于甲醇，在室温下以镍催化氢化，得异丙喘宁。