Van Zwieten P A
Division of Pharmacotherapy, University of Amsterdam, Academic Medical Center, The Netherlands.
Am Heart J. 1988 Nov;116(5 Pt 2):1384-92. doi: 10.1016/0002-8703(88)90128-7.
This survey covers the classification and subdivisions of alpha- and beta-adrenoceptors, including alpha 1 and alpha 2, beta 1 and beta 2, and pre-and postsynaptic receptor subtypes, together with the distribution and functional relevance of the various adrenoceptor subtypes. The emphasis will be on their relevance in circulatory regulatory processes, especially those of the blood vessels. The alpha- and beta-adrenoceptor antagonists that interact with various receptor subtypes are briefly discussed. The control of alpha 2-adrenoceptors concerned with blood pressure regulation is an important target for centrally acting antihypertensive drugs (such as clonidine or alpha-methyldopa). Changes in adrenoceptor density, particularly the down-regulation of beta 1- adrenoceptors (but not beta 2), are found in congestive heart failure. However, the experimental findings about alpha-and beta-adrenoceptors in essential hypertension remain controversial. Finally, the influence of alpha- and beta-adrenoceptor antagonists on plasma lipids and carbohydrate metabolism is briefly reviewed. The changes found may be only partly explained on the basis of alpha- or beta-receptor blockade.
本综述涵盖了α和β肾上腺素能受体的分类及亚类，包括α1和α2、β1和β2，以及突触前和突触后受体亚型，同时还涉及了各种肾上腺素能受体亚型的分布及其功能相关性。重点将放在它们在循环调节过程中的相关性上，尤其是在血管方面。文中简要讨论了与各种受体亚型相互作用的α和β肾上腺素能受体拮抗剂。与血压调节相关的α2肾上腺素能受体的控制是中枢性抗高血压药物（如可乐定或α-甲基多巴）的重要作用靶点。在充血性心力衰竭中可发现肾上腺素能受体密度的变化，尤其是β1肾上腺素能受体（而非β2）的下调。然而，关于原发性高血压中α和β肾上腺素能受体的实验结果仍存在争议。最后，简要回顾了α和β肾上腺素能受体拮抗剂对血浆脂质和碳水化合物代谢的影响。所发现的变化可能仅部分基于α或β受体阻滞来解释。
