近年来,阿片样物质一直引起科学家的极大关注,其中一个重要原因是希望找到新型强效镇痛药且没有吗啡那样的成瘾性。由于吗啡作用于μ受体,因此寻找新型镇痛药的依据是了解非μ受体,尤其是κ受体介导的镇痛的特点。已有充分证据表明,κ受体确实参与镇痛,但κ激动剂的一些特性阻碍其开发利用。首批选择性κ激功剂已进入临床试验阶段。 In recent years, opioids have drawn great attention from scientists. One of the important reasons for this is the desire to find new potent analgesics without the addictive nature of morphine. Because morphine acts on μ receptors, the search for new analgesics is based on the understanding of non-μ receptors, especially κ receptor-mediated analgesia. There is good evidence that kappa receptor does participate in analgesia, but some of the properties of kappa agonists prevent its development. The first selective kappa agonist has entered the clinical trial phase.