Progress in the clinical application of the biased μ-opioid agonist olic-eridine

VernacularTitle:偏向性μ-阿片受体激动剂奥赛利定的临床应用进展
Author: Changmao ZHU ¹ ; Li XIE ; Zifeng WU ; Sen WANG ; Qi ZHANG ; Xiangqing XU ; Chun YANG
Author Information

1. 南京医科大学第一附属医院麻醉与围术期医学科,南京 210029,江苏
Keywords: oliceridine(TRV-130); pharmacologi-cal mechanism; clinical application; adverse reac-tions
From: Chinese Journal of Clinical Pharmacology and Therapeutics 2024;29(9):1057-1061
CountryChina
Language:Chinese
Abstract: Opioid receptors μOR,δOR,κOR and NOPR are all G protein-coupled receptors(GPCRs),which mainly function through G protein and β-ar-restin.Recent studies have found that G protein mediates analgesia,while β-arrestin reduces anal-gesia and is related to the side effects of opioids.Oliceridine is the first biased μOR agonist approved for commerce.It mainly exerts analgesic effect by activating G protein.It has rapid onset of action and reliable analgesic effect.Due to its low activity on β-arrestin,the incidence of side effects is low,comparing to the classic opioid morphine.Oliceri-dine can be safely used in patients with liver or kid-ney insufficiency and its metabolite is inactive.This article summarizes the current progress of pharma-cological research and clinical application of oliceri-dine,aiming to provide reference for the clinical practice of oliceridine.