阿片受体的病理生理研究进展

Study progress in opioid receptor pathophysiology

阿片受体属G蛋白偶联受体,其配体是阿片肽物质。阿片受体在人体内广泛存在,有着复杂的生物学效应,除了既往研究比较多的镇痛、耐受、成隐机制以及对神经系统的影响和呼吸抑制的效应外,其对心血管循环系统、免疫系统等也有着很重要的影响。阿片受体有许多亚型,最常见的三种经典阿片受体为μ、δ、κ受体,它们各自有其特异的内源性配体,发挥不同的生物效应。应激状态下,内啡肽的升高成为纳洛酮在急危重症的应用基础。对阿片受体生物效应的深入研究有助于更进一步明确纳洛酮的药理机制,为开发特异性阿片受体阻断剂和激动剂提供理论基础。

Opioid receptor is G protein-coupled receptor and its ligand is opioid peptide. Opioid receptor occurs widely in the body and has complex biological effects. Apart from the mechanism about analgesia, toleration and addiction, inhibition of respiration and influence on nervous system that had been studied intensively before, opioid system also has important effects on cardiovascular system and immunologic system. Opioid receptor family consist of a lot of subtypes, among which the three most classical types axe μ receptor, δ receptor and κ receptor. Each of them has their own endogenous ligand and functions respectively. In the condition of stress, increase of endorphins is the theoretical principle for naloxone application. The intensive study of the biological effect of opioid receptor will serve for further defining the pharmacological mechanism of naloxone and provide theory basis for development of opioid agonist and antagonist.