Dezocine Exerts Analgesic Effects in Chronic Pain by Activation of κ- and μ-Opioid Receptors and Inhibition of Norepinephrine and Serotonin Reuptake
文献类型：期刊论文
| 作者 | Liu, Zihan1,2,3; Liu, Anan1,2,3; Chen, Jing2 ; Chai, Jing-Rui2; Liu, Panwen1,2; Ye, Ru-Feng2; Liu, Jing-Gen2,3,4; Wang, Yu-Jun1,2,3
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| 刊名 | PAIN RESEARCH & MANAGEMENT
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| 出版日期 | 2025 |
| 卷号 | 2025期号:1页码:9 |
| 关键词 | analgesic chronic pain dezocine norepinephrine reuptake opioid receptor serotonin reuptake |
| ISSN号 | 1203-6765 |
| DOI | 10.1155/prm/5656675 |
| 通讯作者 | Liu, Jing-Gen(jgliu@simm.ac.cn) ; Wang, Yu-Jun(yjwang@simm.ac.cn) |
| 英文摘要 | Background: Dezocine is a leading analgesic in China used for relieving moderate to severe pain. Previous studies have characterized its pharmacological properties, demonstrating its role as a partial agonist at both the kappa-opioid receptor (KOR) and the mu-opioid receptor (MOR), thereby producing potent antinociceptive effects in acute pain models. However, its efficacy and mechanisms in chronic pain management remained unclear. Methods: Chronic pain models, including chronic neuropathic pain and cancer pain, were employed using chronic constriction injury (CCI) of the sciatic nerve and bone cancer pain (BCP) methodologies, respectively. The assessment of the mechanical allodynia was conducted using a von Frey filament. Results: Dezocine, administered via the intraperitoneal route, alleviated both neuropathic pain and cancer pain in a dose-dependent manner, with ED50 of 1.3 mg/kg and 1.6 mg/kg, respectively. In the CCI model, the analgesic effect of dezocine was significantly inhibited by pretreating with KOR antagonist nor-BNI, MOR antagonist beta-FNA, alpha 2-adrenoceptor antagonist yohimbine, and 5-HT2A receptor antagonist altanserin. In the BCP model, dezocine-induced analgesia was markedly suppressed by nor-BNI, beta-FNA, and yohimbine but not altanserin. Conclusion: These results suggest that, in neuropathic pain, the analgesic effects of dezocine are mediated through KOR and MOR activation, together with norepinephrine reuptake inhibition (NRI) and serotonin reuptake inhibition. In contrast, in cancer pain, KOR and MOR activation and NRI are involved in mediating the analgesic effect of dezocine. This study, along with previous data, enhances our understanding of the potential clinical utility of dezocine and elucidates its mechanisms of action in chronic pain management. |
| WOS关键词 | CHRONIC CONSTRICTION INJURY ; NEUROPATHIC PAIN ; RAT MODEL ; ANTAGONIST ; EXPRESSION ; TAPENTADOL |
| 资助项目 | Science & Technology Innovation and Development Plan in Yantai City |
| WOS研究方向 | Neurosciences & Neurology |
| 语种 | 英语 |
| WOS记录号 | WOS:001459457800001 |
| 出版者 | WILEY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/316929]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Liu, Jing-Gen; Wang, Yu-Jun |
| 作者单位 | 1.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 4.Zhejiang Chinese Med Univ, Sch Pharmaceut Sci, Hangzhou 310053, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Zihan,Liu, Anan,Chen, Jing,et al. Dezocine Exerts Analgesic Effects in Chronic Pain by Activation of κ- and μ-Opioid Receptors and Inhibition of Norepinephrine and Serotonin Reuptake[J]. PAIN RESEARCH & MANAGEMENT,2025,2025(1):9. |
| APA | Liu, Zihan.,Liu, Anan.,Chen, Jing.,Chai, Jing-Rui.,Liu, Panwen.,...&Wang, Yu-Jun.(2025).Dezocine Exerts Analgesic Effects in Chronic Pain by Activation of κ- and μ-Opioid Receptors and Inhibition of Norepinephrine and Serotonin Reuptake.PAIN RESEARCH & MANAGEMENT,2025(1),9. |
| MLA | Liu, Zihan,et al."Dezocine Exerts Analgesic Effects in Chronic Pain by Activation of κ- and μ-Opioid Receptors and Inhibition of Norepinephrine and Serotonin Reuptake".PAIN RESEARCH & MANAGEMENT 2025.1(2025):9. |
入库方式： OAI收割
来源：上海药物研究所
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