Berlan M, Montastruc J L, Lafontan M
Department of Medical and Clinical Pharmacology, Faculty of Medicine, Toulouse, France.
Trends Pharmacol Sci. 1992 Jul;13(7):277-82. doi: 10.1016/0165-6147(92)90085-k.
The discovery of various alpha 2-adrenoceptor subtypes in numerous tissues and studies of alpha 2-adrenoceptor-mediated mechanisms has generated considerable interest in their physiological functions. It has also increased possibilities for the design of new pharmacological tools and for the study of the pharmacological impact of new drugs. Alpha 2-adrenoceptors are located pre- and postsynaptically both in the central noradrenergic pathways and on the autonomic nerve endings. It is difficult to dissociate alpha 2-adrenoceptor-mediated autoregulation, involving presynaptic receptors, from actions dependent on post- and extrajunctional alpha 2-adrenoceptor activation. A lot of alpha 2-adrenoceptors are subject to permanent tonic activation by the sympathetic nervous system. Max Lafontan and colleagues review the major actions of alpha 2-adrenoceptors and consider the sites of impact of alpha 2-antagonists that could initiate further research for putative applications of these drugs. Many of the possible targets for alpha 2-adrenoceptor antagonists have not yet been explored clinically.
在众多组织中发现了多种α2 -肾上腺素能受体亚型，并对α2 -肾上腺素能受体介导的机制进行了研究，这引发了人们对其生理功能的浓厚兴趣。这也增加了设计新药理学工具以及研究新药药理学影响的可能性。α2 -肾上腺素能受体位于中枢去甲肾上腺素能途径的突触前和突触后，以及自主神经末梢。涉及突触前受体的α2 -肾上腺素能受体介导的自动调节，很难与依赖于突触后和接头外α2 -肾上腺素能受体激活的作用区分开来。许多α2 -肾上腺素能受体受到交感神经系统的持续紧张性激活。马克斯·拉方丹及其同事综述了α2 -肾上腺素能受体的主要作用，并考虑了α2 -拮抗剂的作用位点，这可能会引发对这些药物潜在应用的进一步研究。α2 -肾上腺素能受体拮抗剂的许多可能靶点尚未进行临床研究。
