Dezocine as a potent analgesic:overview of its pharmacological characterization  

作　　者：Rong-Rong Ye Shuang Jiang Xu Xu Yan Lu Yu-Jun Wang Jing-Gen Liu 

机构地区：[1]School of Chemical and Environmental Engineering,Shanghai Institute of Technology,Shanghai 201418,China [2]CAS Key Laboratory of Receptor Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China [3]School of Chinese Materia Medica,Nanjing University of Chinese Medicine,Nanjing 210023,China

出　　处：《Acta Pharmacologica Sinica》2022年第7期1646-1657,共12页中国药理学报（英文版）

基　　金：The research was supported by the National Natural Science Foundation of China(81671322 to JGL and 81773710 to YJW);the Youth Innovation Promotion Association of the Chinese Academy of Sciences(2017334 to YJW).

摘　　要：Dezocine,a synthetic opioid,introduced in 1970s as an analgesic,was redeveloped for relieving moderate to severe pain by Yangtze River Pharmaceutical Group in China in 2009.To date,dezocine occupies 45%of China’s opioid analgesic market.Along with dezocine being a dominated painkiller,a certain amount of research was conducted to elucidate dezocine’s action.In this review we summarize the current knowledge on the receptor,preclinical and clinical pharmacology of dezocine.Briefly,preclinical data show that dezocine is effective under varying pain conditions,particularly chronic neuropathic pain and cancer pain,through activation of opioid receptors,and inhibition of norepinephrine reuptake.Clinical data establish the effectiveness of dezocine either as a primary analgesic for postoperative pain management or a supplement for balanced analgesia.The receptor profile of dezocine is different from known pureμagonists,and allows it to be used in combination with other opioids for additivity in efficacy or lower incidence of adverse effects.

关 键 词：DEZOCINE opioid receptors NOREPINEPHRINE serotonin transporter postoperative pain ANESTHESIA 

分 类 号：R96[医药卫生—药理学]