Kappa-opioid Receptors and Analgesia

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.