Ligand bias prevents class equality among beta-blockers.
Ligand bias prevents class equality among beta-blockers.
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DOI：
10.1016/j.coph.2014.03.002
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发表时间：
2014-06
影响因子：
4
通讯作者：
Bond R
中科院分区：
文献类型：
--
作者：
Thanawala VJ;Forkuo GS;Stallaert W;Leff P;Bouvier M;Bond R
β阻滞剂被用于从高血压到青光眼等多种疾病。在一些疾病/情况下，所有的β阻滞剂都是有效的，而在另一些疾病/条件下，只有某些亚群在治疗上是有益的。仅有一小部分β阻滞剂显示临床疗效的最好记录的例子是心力衰竭，这一类别的成员从完全无效到治疗这种疾病的首选药物。同样，β阻滞剂在小鼠哮喘模型和两项试验性临床研究中进行了测试。另一个不同的亚组被发现对这一临床适应症有效。这些发现对目前对这些药物进行分类的系统提出了质疑。当考虑到β阻滞剂的严格药理学定义和适当的临床应用时，将其视为单一类别是具有误导性的。
β-blockers are used for a wide range of diseases from hypertension to glaucoma. In some diseases/conditions all β-blockers are effective, while in others only certain subgroups are therapeutically beneficial. The best-documented example for only a subset of β-blockers showing clinical efficacy is in heart failure, where members of the class have ranged from completely ineffective, to drugs of choice for treating the disease.. Similarly, β-blockers were tested in murine asthma models and two pilot clinical studies. A different subset was found to be effective for this clinical indication. These findings call into question the current system of classifying these drugs. To consider “β-blockers”, as a single class is misleading when considering their rigorous pharmacological definition and their appropriate clinical application.