摘要
前列腺素E_(2)(prostaglandinE_(2),PGE_(2))是花生四烯酸代谢产生的重要脂质分子,在多种生理和病理活动中发挥重要作用。非甾体抗炎药(non-steroidal anti-inflammatory drugs,NSAIDs)主要通过抑制PGE_(2)的生成而被广泛用于各类炎症性疾病的治疗和发热、疼痛症状的缓解。PGE_(2)功能的发挥主要依赖于与4种不同的G蛋白耦联受体相结合,其中PGE_(2)受体亚型1(PGE_(2)receptor1,EP1)的分布相对比较局限,且PGE_(2)与EP1的亲和力相对较低。尽管如此,EP1在心血管、泌尿、消化等系统的生理功能维持和稳态调节方面却发挥重要作用。此外,EP1广泛参与炎症反应、痛觉维持和多系统的病理生理学功能调节。本文拟就近年来有关EP1在生理和病理生理学方面的功能和研究现状,以及与之相关药物的研究进展进行简要综述。
Prostaglandin E_(2)(PGE_(2))is an important lipid molecule derived from arachidonic acid,which regulates a variety of physiological and pathological activities.Based on the inhibition of inflammatory PGE_(2)production,non-steroidal anti-inflammatory drugs(NSAIDs)are considered as the most commonly used drugs to treat inflammatory diseases and to relieve fever and pain symptoms.PGE_(2)mediates its functions via four different G protein-coupled receptors,named EP1–EP4.Though the limited distribution and low PGE_(2)affinity of EP1,it plays important roles in the maintenance of many physiological functions and homeostasis.Moreover,EP1 is widely involved in the inflammatory response,pain perception and multisystem pathological function regulation.In this review,we will briefly summarize the recent advances on the physiological and pathophysiological function of EP1 and its targeted drugs development.
作者
陈书涛
季爽
郭美娜
陈丽红
CHEN Shu-Tao;JI Shuang;GUO Mei-Na;CHEN Li-Hong(College of Basic Medical Sciences,Dalian Medical University,Dalian 116044,China;Advanced Institute for Medical Sciences,Dalian Medical University,Dalian 116044,China)
出处
《生理学报》
CAS
CSCD
北大核心
2024年第1期105-118,共14页
Acta Physiologica Sinica
基金
supported by the National Natural Science Foundation of China(No.32071157,31900142)
Liaoning Science and Technology Department Program,China(No.2020-BS-202)。
