神经肽S的功能与构效关系研究进展  

PROGRESS IN THE STUDIES OF FUNCTIONS AND STRUCTURE-ACTIVITY RELATIONSHIP OF NEUROPEPTIDE S

作　　者：常民[1] 彭雅丽[1] 李威[1] 王锐[1,2] 

机构地区：[1]兰州大学生命科学学院,生物化学与分子生物学研究所,兰州730000 [2]兰州大学基础医学院,甘肃省新药临床前研究重点实验室,兰州730000

出　　处：《生物物理学报》2009年第3期175-182,共8页Acta Biophysica Sinica

基　　金：国家自然科学基金项目(90813012;30600094)~~

摘　　要：神经肽S(neuropeptide S,NPS)是通过反向药理学策略鉴定的由20个氨基酸组成的新神经肽,它激活G蛋白偶联受体(NPSR)而发挥作用。NPS及其受体主要分布于中枢上与觉醒和应激相关的脑区。目前的研究表明NPS系统具有广泛的生理作用,如增加觉醒、抑制睡眠、抗焦虑作用、抑制摄食和调节免疫功能等,成为相关疾病的一个重要的新药物靶点。同时,研究神经肽S的构效关系并寻找新的高效激动剂和选择性拮抗剂,对揭示其作用机理有重要意义。Neuropeptide S （NPS）, a new peptide possessing 20 amino acid residues, was identified recently via the reverse pharmacology approach. NPS selectively binds and activates an orphan G-protein coupled receptor, named NPS receptor （NPSR）, which is also known as GPR154 or GPRA. NPS and NPS receptor mRNA are expressed in the brain regions, which were thought to modulate wakefulness and anxiety. NPS and the cognate receptor have been shown to modulate many physiological and pathological activities. NPS administered centrally in rodents produces a wide range of biological effects including stimulation of wakefulness, hyperlocomotion, inhibition of food intake, anxiolytic-like effects and immunomodulatory effect. NPS system may provide a potential target for pharmacological treatment of related diseases. It is important to study the structure-activity relationship of NPS for understanding physiological roles of NPS/NPSR system.

关 键 词：神经肽S 神经肽S受体 觉醒 抗焦虑 构效关系 

分 类 号：Q5[生物学—生物化学]