孤啡肽受体的配体研究进展

Progress in The Studies of Ligands for Nociceptin Receptor

孤啡肽 (nociceptin或orphaninFQ)发现于 1 995年底 ,它是阿片受体样受体 (ORL1或LC 1 32 )的内源性配体 ,在痛觉调节、心血管系统、离子通道、依赖和耐受、学习和记忆等方面具有广泛的生物学活性 .最近几年 ,对孤啡肽受体与相关配体构效关系的研究成为一个新的热点 .对在研究构效关系过程中所发现的孤啡肽受体相关配体 (片段、拮抗剂、激动剂、部分激动剂和阻断剂 )的研究情况进行了介绍 .

Nociceptin was discovered at the end of 1995. It is the endogenous ligand of opioid receptor like 1 (ORL1 or LC 132) receptor. It plays an important role in pain modulation, cardiovascular system, ion channel, dependence and tolerance, learning and memory, etc . It is becoming a new research field to investigate the structure activity relationship of ORL1 receptor and its ligands in recent years. Now, the studies on NC fragments, agonists, partial agonists, and antagonists that were found in the course of investigating the structure activity relationship of nociceptin are reviewed.