Millan M J
Fondax, Neurobiology Division, Groupe de Recherches Servier, Paris, France.
Trends Pharmacol Sci. 1990 Feb;11(2):70-6. doi: 10.1016/0165-6147(90)90321-x.
Over the past decade, opioids have attracted great attention. One important reason for this is the need for novel, strong analgesics free of the abuse potential and side-effects of narcotics such as morphine. Because morphine acts at mu-opioid receptors, efforts have been made to characterize analgesia mediated by non-mu sites, in particular kappa-opioid receptors. There is now good evidence that kappa-receptors do indeed mediate analgesia. However, kappa-agonists display properties that could curtail their therapeutic exploitation. Since the first selective kappa-agonists are now entering clinical trials, this is an opportune moment for Mark Millan to review the pharmacology of drugs of this type in the control of nociception and their therapeutic potential as analgesics.
在过去十年中，阿片类药物备受关注。其中一个重要原因是需要新型强效镇痛药，这类药物没有吗啡等麻醉药品的滥用可能性和副作用。由于吗啡作用于μ-阿片受体，人们已努力对由非μ位点介导的镇痛作用进行表征，尤其是κ-阿片受体。现在有充分证据表明κ-受体确实介导镇痛作用。然而，κ-激动剂具有的一些特性可能会限制其在治疗中的应用。鉴于首批选择性κ-激动剂现已进入临床试验阶段，马克·米兰在此恰当时机对这类药物在控制伤害感受方面的药理学及其作为镇痛药的治疗潜力进行了综述。
