通过比索洛尔和阿替洛尔对特布他林输注引起的脂解反应的影响来评估它们的β1选择性。
Assessment of beta-1 selectivity of bisoprolol and atenolol by means of their influence on the lipolytic response to an infusion of terbutaline.
作者信息
Kendall M J, Akhlaghi S, Haffner C A
机构信息
Department of Clinical Pharmacology, Medical School, Edgbaston, Birmingham, U.K.
出版信息
J Clin Pharm Ther. 1991 Feb;16(1):25-9. doi: 10.1111/j.1365-2710.1991.tb00280.x.
We have investigated the beta-1 selectivity of a new beta-blocker, Bisoprolol, by comparing its effect on lipolysis induced by intravenous terbutaline infusion with that of Atenolol. At a dose of 5 mg, Bisoprolol had virtually no beta-2 blocking activity as measured by free fatty acid (FFA) release during terbutaline infusion. At a dose of 10 mg, Bisoprolol had a small but statistically insignificant effect on FFA release similar to 50 mg Atenolol. At a dose of 20 mg, Bisoprolol had significant beta-2 blocking activity. At lower doses, therefore, Bisoprolol is a very selective beta-blocker.
我们通过比较新型β受体阻滞剂比索洛尔与阿替洛尔对静脉输注特布他林诱导的脂肪分解的影响，研究了比索洛尔的β1选择性。在5毫克的剂量下，通过特布他林输注期间游离脂肪酸（FFA）的释放测定，比索洛尔几乎没有β2阻断活性。在10毫克的剂量下，比索洛尔对FFA释放有轻微但无统计学意义的影响，类似于50毫克阿替洛尔。在20毫克的剂量下，比索洛尔具有显著的β2阻断活性。因此，在较低剂量下，比索洛尔是一种非常有选择性的β受体阻滞剂。
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