基于阿片受体亚型的药物研究进展

Research progress in drugs based on opioid receptor subtypes

作为一类经典镇痛药物,阿片类药物在临床广泛使用。已有大量研究阐述了阿片受体的功能,除调节疼痛、依赖和情绪外,阿片受体还介导多种生理效应,影响机体正常生理及病理活动。已发现4种主要的阿片受体亚型(μ,δ,κ和ORL1),它们在作用特点和脑区分布上存在显著差异,这决定了其所介导生物效应的不同。基于阿片受体不同亚型功能的差异,开发相应特异性靶向药物已成为药物研发的新方向。本文综述了基于阿片受体亚型的药物研究进展,并展望了其发展前景。

As classic analgesic drugs, opioids have received much attention in the medical area. With better clarified functions of opioid receptors, they are confirmed to mediate pain, addiction, emotion, and a variety of physiological and pathological activities. So far, opioid receptors have been divided in- to four subtypes including μ,δ,κ, and ORL1 receptor. It has been proved that μ,δ and κ opioid receptor subtypes can induce different effects due to their own role and their distribution in the central nervous system. Based on the effect of opioid receptor subtypes, the development of specific drugs has become a new area in drug research. This paper summarizes research progress regarding those drugs, and developments are also predicted.