α2肾上腺素受体激动剂的研究进展

Advances in research of α-AR agonists

α2肾上腺素受体(α2-AR)是一类G蛋白偶联受体,具有3种不同组织分布与生物功能的受体亚型。α2-AR激动剂能够产生一定的镇痛和镇静作用,当与麻醉剂联合应用时可减少临床手术中麻醉药物的用量。近年来,针对肾上腺素和右美托咪定等药物的基本骨架研发出大量具有高活性和选择性的苯乙胺类和咪唑环类α2-AR激动剂。本文综述了α2肾上腺素受体及其激动剂的研究进展,为研发新一代高效、高选择性α2-AR激动剂提供参考。

Alpha 2 adrenergic receptor( α2-AR) is a type of G protein coupled receptors( GPCRs),and it has three receptor subtypes w ith different tissue distribution and biological functions. α2-AR agonists have analgesic and sedative effects,w hich make them specially useful in association w ith anesthetics to reduce the dosage of anesthetics in clinical surgery. In recent years,a large number of highly active and selective phenylethylamines and imidazoles α2-AR agonists based on the structures of adrenaline and dexmedetomidine had been found. In this paper,w e review ed the advances of α2-AR and agonists to provide a reference for developing a new generation of efficient and selective α2-AR agonists.