Piascik M T, Soltis E E, Piascik M M, Macmillan L B
Department of Pharmacology, University of Kentucky College of Medicine, Lexington 40536, USA.
Pharmacol Ther. 1996;72(3):215-41. doi: 10.1016/s0163-7258(96)00117-9.
This manuscript is intended to provide a comprehensive review of the alpha-adrenoceptors (ARs) and their role in vascular regulation. The historical development of the concept of receptors and the division of the alpha-ARs into alpha 1 and alpha 2 subtypes is traced. Emphasis will be placed on current understanding of the specific contribution of discrete alpha 1- and alpha 2-AR subtypes in the regulation of the vasculature, selective agonists and antagonists for these receptors, the second messengers utilized by these receptors, the myoplasmic calcium pathways activated to initiate smooth muscle contraction, as well as the clinical uses of agonists and antagonists that work at these receptors. New information is presented that deals with the molecular aspects of ligand interactions with specific subdomains of these receptors, as well as mRNA distribution and the regulation of alpha 1- and alpha 2-AR gene transcription and translation.
本手稿旨在全面综述α-肾上腺素能受体（ARs）及其在血管调节中的作用。追溯了受体概念的历史发展以及α-ARs分为α1和α2亚型的过程。将重点阐述目前对不同α1-和α2-AR亚型在血管系统调节中的具体作用、这些受体的选择性激动剂和拮抗剂、这些受体利用的第二信使、激活以引发平滑肌收缩的肌浆钙途径，以及作用于这些受体的激动剂和拮抗剂的临床应用的理解。还介绍了有关配体与这些受体特定亚结构域相互作用的分子方面、mRNA分布以及α1-和α2-AR基因转录和翻译调控的新信息。
