Colucci W S
Am J Cardiol. 1983 Feb 24;51(4):639-43. doi: 10.1016/s0002-9149(83)80201-x.
The vascular postsynaptic alpha 1 receptor is the major locus through which adrenergically determined vascular tone is mediated. Therefore, blockade of this receptor is a particularly specific approach to the major pathophysiologic defect in hypertension--an elevation of peripheral vascular resistance. Although the mechanism responsible for this increase in peripheral vascular resistance in hypertension is not known, it is apparent that the sympathetic nervous system plays a key role. In addition, considerable evidence suggests that a common abnormality in hypertension is an increase in the sensitivity of vessels to alpha-adrenergic stimulation, a defect potentially located at the alpha-receptor level. Basic radioligand binding studies of vascular alpha 1 receptors, in fact, demonstrate that the affinity, or avidity, of binding of these sites is under the regulation of both neural and humoral factors. Although diuretics, and more recently, beta-adrenergic blocking agents, have been utilized for the initial treatment of hypertension, recent information about the adverse effects of these agents has led to a reappraisal of the role of alpha-receptor blockade as a rational approach to the initial treatment of hypertension.
血管突触后α1受体是介导肾上腺素能决定的血管张力的主要位点。因此，阻断该受体是针对高血压主要病理生理缺陷——外周血管阻力升高的一种特别特异性的方法。虽然高血压中外周血管阻力增加的机制尚不清楚，但很明显交感神经系统起着关键作用。此外，大量证据表明，高血压的一个常见异常是血管对α-肾上腺素能刺激的敏感性增加，这一缺陷可能位于α-受体水平。事实上，血管α1受体的基础放射性配体结合研究表明，这些位点结合的亲和力或avidity受神经和体液因素的调节。虽然利尿剂以及最近的β-肾上腺素能阻滞剂已被用于高血压的初始治疗，但关于这些药物不良反应的最新信息导致人们重新评估α-受体阻断作为高血压初始治疗合理方法的作用。
