摘要
多肽在机体中具有重要的生理功能,并且它具有化学合成和修饰的便利性,因此吸引了越来越多的化学、生物学及其交叉领域研究人员的研究兴趣。神经肽FF(NPFF)作为阿片调节肽在阿片耐受等药理学方面具有重要的调节作用。然而迄今为止仍缺乏NPFF受体高选择性的激动剂和拮抗剂,从而阻碍了NPFF药理学功能及其作用机制的研究。本文简述了NPFF的发现,综述了近几年来在NPFF的前体、受体和生理学功能等方面所取得的最新进展。结合本实验室的工作,重点介绍了NPFF构效关系方面的研究,并展望了该研究方向今后的发展趋势。
Peptides play pivotal roles in controlling and modulating the physiological functions. More and more attention has focused on the subject of peptides due to its facilities of chemical synthesis and modification. Neuropeptide FF （NPFF）, an important opioid-modulating peptide, mediates a variety of biological actions, such as opioid tolerance and abstinence. However, to date, the potent and highly selective agonists and antagonists for NPFF receptors are still lacking, which hamper studies of the pharmacological activities of NPFF. This paper introduces the finding of NPFF, and reviews the progress on the precursors, the receptors and the bio-activities of NPFF in recent years. The structrueactivitiy relationship studies of NPFF are especially described. Authors＇ work in studying of the effects of chemical modifications of NPFF on the pharmacological activities is referred. The research trends for the future are proposed.
出处
《化学进展》
SCIE
CAS
CSCD
北大核心
2007年第12期1977-1985,共9页
Progress in Chemistry
基金
国家杰出青年科学基金(No.20525206)
教育部"长江学者"特聘教授项目资助
关键词
神经肽FF
受体
构效关系
激动剂
拈抗剂
neuropeptide FF （NPFF）
receptors
structure-activity relationship
agonists
antagonists
