The 991st Hospital of Joint Logistic Support Force of People's Liberation Army, Xiangyang, China.
Xiangyang No. 4 Middle School Compulsory Education Department, Xiangyang, China.
Medicine (Baltimore). 2024 Jul 19;103(29):e38837. doi: 10.1097/MD.0000000000038837.
Opioids exert analgesic effects by agonizing opioid receptors and activating signaling pathways coupled to receptors such as G-protein and/or β-arrestin. Concomitant respiratory depression (RD) is a common clinical problem, and improvement of RD is usually achieved with specific antagonists such as naloxone; however, naloxone antagonizes opioid analgesia and may produce more unknown adverse effects. In recent years, researchers have used various methods to isolate opioid receptor-mediated analgesia and RD, with the aim of preserving opioid analgesia while attenuating RD. At present, the focus is mainly on the development of new opioids with weak respiratory inhibition or the use of non-opioid drugs to stimulate breathing. This review reports recent advances in novel opioid agents, such as mixed opioid receptor agonists, peripheral selective opioid receptor agonists, opioid receptor splice variant agonists, biased opioid receptor agonists, and allosteric modulators of opioid receptors, as well as in non-opioid agents, such as AMPA receptor modulators, 5-hydroxytryptamine receptor agonists, phosphodiesterase-4 inhibitors, and nicotinic acetylcholine receptor agonists.
阿片类药物通过激动阿片受体并激活与 G 蛋白和/或β-arrestin 等受体偶联的信号通路发挥镇痛作用。同时出现的呼吸抑制(RD)是一个常见的临床问题,通常通过纳洛酮等特异性拮抗剂来改善 RD;然而,纳洛酮拮抗阿片类药物的镇痛作用,并可能产生更多未知的不良反应。近年来,研究人员采用各种方法来分离阿片受体介导的镇痛和 RD,旨在保留阿片类药物的镇痛作用,同时减轻 RD。目前,重点主要放在开发具有较弱呼吸抑制作用的新型阿片类药物或使用非阿片类药物来刺激呼吸。本综述报告了新型阿片类药物(如混合阿片受体激动剂、外周选择性阿片受体激动剂、阿片受体剪接变体激动剂、偏向性阿片受体激动剂和阿片受体别构调节剂)和非阿片类药物(如 AMPA 受体调节剂、5-羟色胺受体激动剂、磷酸二酯酶-4 抑制剂和烟碱型乙酰胆碱受体激动剂)的最新进展。