Lindén A, Rabe K F, Löfdahl C G
Division of Pulmonary Medicine, Sahlgrenska Hospital, University of Gothenburg, Sweden.
Lung. 1996;174(1):1-22. doi: 10.1007/BF00167947.
The mechanisms behind the long duration of bronchodilating action of the beta 2-adrenoceptor agonists formoterol and salmeterol are only partially understood. This review compares pharmacological characteristics of long-acting versus short-acting beta 2-adrenoceptor agonists in human and animal airways. Based upon the reviewed evidence, it is concluded that for beta 2-adrenoceptor agonists, long duration of action may depend upon several factors. Both formoterol and salmeterol display a higher lipophilicity and have a higher affinity, selectivity, and potency than most short-acting agonists at the beta 2-adrenoceptor. Of these factors, lipophilicity may prove to be one of the most important ones by determining the amount of drug entering into the cell membrane in the vicinity of the beta 2-adrenoceptor. However, the receptor affinity, maximal relaxant effect (efficacy or intrinsic activity), potency, and receptor selectivity may also be of importance in determining how much beta 2-adrenoceptor agonist must remain at the receptor for sustained action.
β2肾上腺素能激动剂福莫特罗和沙美特罗具有长效支气管扩张作用，但其背后的机制仅得到部分理解。本综述比较了长效与短效β2肾上腺素能激动剂在人和动物气道中的药理学特性。基于所审查的证据，得出结论：对于β2肾上腺素能激动剂，作用持续时间长可能取决于几个因素。福莫特罗和沙美特罗均表现出较高的亲脂性，并且在β2肾上腺素受体上比大多数短效激动剂具有更高的亲和力、选择性和效能。在这些因素中，亲脂性可能是最重要的因素之一，因为它决定了进入β2肾上腺素受体附近细胞膜的药物量。然而，受体亲和力、最大舒张效应（效能或内在活性）、效能和受体选择性在确定需要多少β2肾上腺素能激动剂留在受体上以维持作用方面也可能很重要。
