Bousquet J, Michel F B
Service de Pneumologie, Hôpital l'Aiguelongue, Montpellier.
Rev Mal Respir. 1992;9 Suppl 1:R7-10.
Salmeterol is an original molecule characterized by its long duration of action (greater than 12 hrs in humans). Salmeterol is a highly selective beta-2 agonist that is from 2 to 15 times more potent than salbutamol on beta-2 receptors of bronchial smooth muscle and 10,000 times more potent than isoprenaline on beta-1 receptors. The duration of action of salmeterol on bronchial smooth muscle has been shown to be much superior than all other beta-2 sympathomimetics that have been studied, including formoterol. Salmeterol has two side chains that are linked by a long hydroxycarbon chain. Its long duration of action could be explained by the link to the cell membrane through an exo-site which is distinct from the beta-2 receptor. In vitro and in the animal model, salmeterol has a triple effect: inhibition of the liberation of inflammatory mediators (histamine, prostaglandins, leukotrienes), inhibition of cell influx and of protein extravasation. The relevance of this effect remains to be establish in humans.
沙美特罗是一种原研药物，其特点是作用持续时间长（在人体中超过12小时）。沙美特罗是一种高度选择性的β₂受体激动剂，对支气管平滑肌的β₂受体的作用比沙丁胺醇强2至15倍，对β₁受体的作用比异丙肾上腺素强10000倍。沙美特罗对支气管平滑肌的作用持续时间已被证明比所有其他已研究的β₂拟交感神经药（包括福莫特罗）都要长得多。沙美特罗有两条通过长羟碳链连接的侧链。其作用持续时间长可通过与细胞膜上一个不同于β₂受体的外位点连接来解释。在体外和动物模型中，沙美特罗有三重作用：抑制炎性介质（组胺、前列腺素、白三烯）的释放，抑制细胞内流和蛋白质外渗。这种作用在人体中的相关性仍有待确定。
