van Zwieten P A
Department of Pharmacotherapy and Cardiology, University of Amsterdam, The Netherlands.
J Hypertens Suppl. 1991 Dec;9(6):S18-27.
The rapid development of receptor pharmacology has not only proved to be of great fundamental value, but has also acquired clinical relevance. Major advances have been made in fundamental issues such as the analysis of receptor structures by means of cloning techniques; the elucidation of signal transduction processes, which mediate the signal triggered by receptor activation to intracellular effector structures; and the investigation of receptor changes associated with disease. After a more general discussion of these issues, special attention is paid in the present survey to alpha- and beta-adrenoceptors and to muscarinic receptors. The agonists and antagonists for the various receptor subtypes are discussed, as well as the most important changes in receptor characteristics associated with cardiovascular disease. Potential new therapeutic options based on improved knowledge of receptor pharmacology are discussed for the various alpha- and beta-adrenoceptor subtypes. Special attention is paid to the new and rapidly developing field of muscarinic receptors as a hypothetical basis for drug therapy in cardiovascular and other diseases.
受体药理学的迅速发展不仅已证明具有重大的基础价值,而且还具有临床相关性。在一些基础问题上取得了重大进展,例如通过克隆技术分析受体结构;阐明介导受体激活触发的信号传递到细胞内效应器结构的信号转导过程;以及研究与疾病相关的受体变化。在对这些问题进行更一般性的讨论之后,本次综述特别关注α和β肾上腺素能受体以及毒蕈碱受体。讨论了各种受体亚型的激动剂和拮抗剂,以及与心血管疾病相关的受体特性的最重要变化。针对各种α和β肾上腺素能受体亚型,讨论了基于对受体药理学更深入了解的潜在新治疗选择。特别关注毒蕈碱受体这一迅速发展的新领域,它是心血管疾病和其他疾病药物治疗的一个假设基础。