μ阿片受体激动剂研究进展

Research Progress of μ-Opioid Receptor Agonist

摘要: 上世纪60年代，新型镇痛剂芬太尼的发现引起了各国科学家们对新型镇痛药研究的热潮，人们开始研究吗啡及与吗啡结构相似的芬太尼这类新型镇痛剂的药理作用，生物活性等。自从70年代发现脑内存在阿片受体和内源性阿片肽以来，各国学者都开始积极研究阿片受体的结构。阿片受体主要有μ、δ、κ三种类型，其中，μ受体也是吗啡，芬太尼等镇痛药主要作用的受体蛋白位点。继芬太尼的发现之后，人们又发现了许多其他具有高活性的芬太尼类似物，如羟甲芬太尼(OMF)等。近年来，许多研究都表明敲除δ-阿片受体或者使用阿片类拮抗剂可以减轻或者抑制μ阿片镇痛药长期服用导致的耐受力和药物依赖性。

Abstract: In the 1960s, the discovery of new analgesic fentanyl caused the boom of new analgesic study around the world; people began to study pharmacological effects, biological activity and other characters of the new analgesic of morphine and fentanyl, which is similar to morphine on structure. Since the 1970s, the existence of opioid receptors and endogenous opioid peptides has been found in the brain; many scholars have begun to study the structure of opioid receptor actively. There are mainly three types of opioid receptors (μ, δ, κ), and wherein, μ receptor protein is the primary receptor site of morphine, fentanyl and other analgesics. Following the discovery of fentanyl, many other highly active fentanyl analogs have been found, such as Ohmefentanyl (OMF). Recently, many studies have shown that gene knock-out of δ-opioid receptor or antagonists can reduce or suppress tolerance and drug dependency—the side effects of μ-opioid analgesics for long-term administration.