Chang P C, van Veen S, Vermeij P, van Brummelen P
J Cardiovasc Pharmacol. 1986;8 Suppl 11:S58-60. doi: 10.1097/00005344-198511001-00009.
The beta 1-adrenoceptor selectivity of bisoprolol (BPL) was investigated using the forearm circulation of eight healthy subjects. Each subject was studied twice, with at least 10 days in between each investigation. A brachial artery was cannulated for intra-arterial (i.a.) monitoring of blood pressure and for i.a. infusion of isoproterenol (ISO) and epinephrine (EPI). ISO was given in doses of 0.02-0.10-0.40 and 1.20 ng/kg/min, for 3 min per dose. After 20 min rest, EPI was infused in doses of 0.08 and 2.0 ng/kg/min for 6 min per dose. Subsequently, the subjects received an oral dose of either 20 mg BPL or 100 mg atenolol (ATL), and 2 h later, the ISO and EPI infusions were repeated. Forearm blood flow was measured by venous occlusion strain-gauge plethysmography. ISO produced a dose-dependent vasodilatation, whereas the response to EPI varied between individuals. After administration of BPL and ATL, the ISO dose-response curves were shifted to the right by 2.8 and 2.6 times, respectively (both p less than 0.01). Both beta-blockers influenced the vascular effect of EPI in the direction of vasoconstriction. However, this was only significant for ATL (p less than 0.05). From the latter observation it is concluded that BPL is slightly more beta 1-adrenoceptor-selective than ATL, using the forearm vascular bed.
利用8名健康受试者的前臂循环系统研究了比索洛尔（BPL）的β1 - 肾上腺素能受体选择性。每位受试者接受两次研究，每次研究之间至少间隔10天。通过肱动脉插管进行动脉内（i.a.）血压监测以及异丙肾上腺素（ISO）和肾上腺素（EPI）的动脉内输注。ISO的给药剂量为0.02 - 0.10 - 0.40和1.20 ng/kg/min，每剂持续输注3分钟。休息20分钟后，以0.08和2.0 ng/kg/min的剂量输注EPI，每剂持续6分钟。随后，受试者口服20 mg BPL或100 mg阿替洛尔（ATL），2小时后重复ISO和EPI输注。通过静脉阻断应变片体积描记法测量前臂血流量。ISO产生剂量依赖性血管舒张，而对EPI的反应在个体之间有所不同。给予BPL和ATL后，ISO剂量 - 反应曲线分别右移2.8倍和2.6倍（两者p均小于0.01）。两种β受体阻滞剂均使EPI的血管效应朝血管收缩方向改变。然而，这仅在ATL组具有统计学意义（p小于0.05）。根据后一观察结果得出结论，以前臂血管床作为研究对象时，BPL的β1 - 肾上腺素能受体选择性略高于ATL。
