摘要

BACKGROUND:Salbutamol has been shown to mediate anabolic effects after intravenous administration. However, the mechanism responsible for the anabolic actions of salbutamol remains unknown.
AIM:To investigate the potential mechanism by which salbutamol mediates anabolic effects in vitro.
METHODS:The potential androgenic activity of salbutamol was investigated in vitro by the A-Screen assay that measures androgen-dependent inhibition of proliferation of the androgen receptor (AR)-positive human mammary carcinoma cell line, MCF7-AR1.
RESULTS:The assay was validated with three known androgens; methyltrienolone (R1881), 5alpha-dihydrotestosterone (DHT) and danazol. IC50 values of R1881, DHT and danazol, 4.41x10(-11), 4.44x10(-11) and 1.08x10(-8) M, respectively, were in the ranges known from earlier studies. Our results demonstrate that salbutamol exhibits androgenic activity, with an IC50 value of 8.93x10(-6) M. Anti-estrogenic or cytotoxic effects, which might have interfered with the assay, were excluded by additional experiments on wild-type MCF7 and MCF7-AR1 cells, respectively.
CONCLUSION:These data indicate that salbutamol exerts anabolic effects through androgen receptor agonistic activity in vitro.

译文

背景: 沙丁胺醇已被证明在静脉给药后介导合成代谢效应。然而,沙丁胺醇合成代谢作用的机制仍然未知。
目的: 探讨沙丁胺醇在体外介导合成代谢的潜在机制。
方法: 在体外通过 A-Screen 试验检测雄激素依赖性抑制雄激素受体 (AR) 的增殖,研究沙丁胺醇的潜在雄激素活性。 -阳性人乳腺癌细胞系,MCF7-AR1。
结果: 用三种已知的雄激素验证了该测定; 甲基三烯醇酮 (R1881) 、 5 α-二氢睾酮 (DHT) 和达那唑。R1881 、 DHT 和达那唑的 IC50 值为 4。 41x10 (-11),4。 44x10 (-11) 和 1。 08x10 (-8) M 分别在早期研究中已知的范围内。我们的结果表明沙丁胺醇具有雄激素活性,IC50 值为 8。93x10 (-6) M。对野生型 MCF7 和 MCF7-AR1 细胞的额外实验排除了可能干扰试验的抗雌激素或细胞毒性效应。
结论: 这些数据表明沙丁胺醇通过体外雄激素受体激动活性发挥合成代谢作用。

salbutamol

呼吸 肾上腺素受体激动剂 药物
概述  :  

基本信息 沙丁胺醇化学式为:1-(4-羟基-3-羟甲基苯基)-2-(叔丁氨基)乙醇。分子式为:C13H21NO3。分子量为:239.31。 作用机制沙丁胺醇是一种选择性β2肾上腺素受体激动剂,在治疗剂量下,治疗可逆性气道阻塞疾病,5分钟内快速起效,药效持续4至6小时,其主要作用位于支气管平滑肌上的β2肾上腺素能受体。 适应症沙丁胺醇主要用于缓解哮喘或慢性阻塞性肺部疾患(可逆性气道阻塞疾病)患者的支气管痉挛,及急性预防运动诱发的哮喘,或其他过敏原诱发的支气管痉挛。 禁

salbutamol   /sæl'bjutəmɔl/

       n. 沙丁氨醇,羟甲叔丁肾上腺素;舒喘灵,舒喘宁

       Observe the effect of combined inhalation therapy of salbutamol and Ipratropium Bromide on children with acute asthma episode. 观察沙丁胺醇、溴化异丙托品联合吸入在儿童哮喘急性发作治疗中的疗效。

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