Department of Medicine, New York Medical College/Westchester Medical Center, Valhalla, NY 10595, USA.
J Cardiovasc Pharmacol Ther. 2013 Jul;18(4):310-9. doi: 10.1177/1074248413484986. Epub 2013 Apr 30.
The development and subsequent clinical application of the β-adrenergic receptor blocking drugs represent one of the major advances in human pharmacotherapeutics. No other class of synthetic drugs has demonstrated such widespread therapeutic utility for the treatment and prevention of so many cardiovascular diseases. In addition, these drugs have proven to be molecular probes that have contributed to our understanding of the disease, and on the molecular level, both the structure and function of the 7 transmembrane G protein receptors that mediate the actions of many different hormones, neurotransmitters, and drugs. The evolution of β-blocker drug development has led to refinements in their pharmacodynamic actions that include agents with relative β1-selectivity, partial agonist activity, concomitant α-adrenergic blockers activity, and direct vasodilator activity. In addition, long-acting and ultra-short-acting formulations of β-blockers have also demonstrated a remarkable record of clinical safety in patients of all ages.
β-肾上腺素能受体阻滞剂的发展及其随后在临床上的应用是人类药物治疗学的重大进展之一。没有其他任何一类合成药物能像这类药物一样，对如此众多的心血管疾病的治疗和预防具有如此广泛的治疗作用。此外，这些药物已被证明是分子探针，有助于我们了解疾病，以及在分子水平上，了解介导许多不同激素、神经递质和药物作用的 7 跨膜 G 蛋白受体的结构和功能。β-阻滞剂药物开发的发展导致了它们的药效学作用的改进，包括具有相对β1-选择性、部分激动剂活性、同时具有α-肾上腺素能阻滞剂活性和直接血管扩张活性的药物。此外，长效和超短效β-阻滞剂制剂在所有年龄段的患者中也表现出了显著的临床安全性记录。
