Département de Pharmacologie, Faculté de Médecine, Université de Montréal, Canada.
Mol Brain. 2011 Jun 13;4:25. doi: 10.1186/1756-6606-4-25.
Opiate drugs are the most effective analgesics available but their clinical use is restricted by severe side effects. Some of these undesired actions appear after repeated administration and are related to adaptive changes directed at counteracting the consequences of sustained opioid receptor activation. Here we will discuss adaptations that contribute to the development of tolerance. The focus of the first part of the review is set on molecular mechanisms involved in the regulation of opioid receptor signalling in heterologous expression systems and neurons. In the second part we assess how adaptations that take place in vivo may contribute to analgesic tolerance developed during repeated opioid administration.
阿片类药物是目前最有效的镇痛药，但由于严重的副作用，其临床应用受到限制。这些不良反应中的一些在重复给药后出现，与对抗持续阿片受体激活后果的适应性变化有关。在这里，我们将讨论有助于产生耐受性的适应。综述的第一部分重点介绍了在异源表达系统和神经元中调节阿片受体信号转导的分子机制。在第二部分，我们评估了体内发生的适应性变化如何有助于在反复给予阿片类药物时产生的镇痛耐受。
