Mäki T, Näveri H, Härkönen M, Kontula K
Department of Clinical Chemistry, University of Helsinki, Finland.
Scand J Clin Lab Invest. 1988 Jun;48(4):357-63. doi: 10.3109/00365518809167508.
The effect of peroral propranolol administration on the level of lymphocytic beta-adrenergic receptors was studied in six healthy volunteers using an acute exercise test. When no drug was used, a 15-min ergometer exercise period induced a significant increase in the receptor density (from 42 +/- 5 to 117 +/- 14 fmol/mg protein; mean +/- SEM), followed by a return to the pre-exercise level after a 1-hr rest. During propranolol administration (40 mg, three times daily), the basal receptor level (49 +/- 4 fmol/mg protein) did not change but the exercise-induced increment of the receptor density was significantly inhibited (peak value 79 +/- 5 fmol/mg protein, p less than 0.05). This effect could not be explained by direct competition for receptor binding sites by propranolol nor by differences in the plasma adrenalin and noradrenaline concentrations during the two tests. The fact that propranolol interferes with the normal adaptation of the beta-adrenergic receptor level to acute exercise may explain some of the adverse effects of beta-blocking drugs on physical performance.
在六项健康志愿者中，通过急性运动试验研究了口服普萘洛尔对淋巴细胞β-肾上腺素能受体水平的影响。在未使用药物时，15分钟的测力计运动期可使受体密度显著增加（从42±5增至117±14 fmol/mg蛋白质；平均值±标准误），随后经过1小时休息后恢复至运动前水平。在服用普萘洛尔期间（40毫克，每日三次），基础受体水平（49±4 fmol/mg蛋白质）未发生变化，但运动诱导的受体密度增加受到显著抑制（峰值为79±5 fmol/mg蛋白质，p<0.05）。这种效应既不能用普萘洛尔对受体结合位点的直接竞争来解释，也不能用两次试验期间血浆肾上腺素和去甲肾上腺素浓度的差异来解释。普萘洛尔干扰β-肾上腺素能受体水平对急性运动的正常适应性这一事实，可能解释了β受体阻滞剂对身体性能的一些不良影响。
