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内皮素-1在疼痛中的作用及机制研究进展

胡丛坤¹, 尤浩军^1,2, 雷静^1,2,*

¹延安大学感觉与运动转化医学研究中心，延安 716000；²延安市运动康复医学重点实验室，延安 716000

摘要

内皮素-1是一种源自内皮细胞的多肽，由21个氨基酸残基组成。近年来，研究发现内皮素-1不仅在血管紧张调节中发挥关键作用，还参与包括炎性痛、神经病理性疼痛、癌痛等多类型病理性痛的发生与发展。内皮素-1通过与其受体结合，激活多种信号通路，包括蛋白激酶C、钙离子通道和磷酸肌醇途径等，进而影响神经元的兴奋性和伤害性信息传递。本文通过综述目前内皮素-1在疼痛发生和发展中的作用和机制及常用的内皮素-1 受体抑制剂，为更好地利用内皮素-1 及其受体缓解与治疗病理性痛提供线索。

关键词： 内皮素-1; 疼痛; 内皮素受体

Research progress on the role and mechanism of endothelin-1 in pain

HU Cong-Kun¹, YOU Hao-Jun^1,2, LEI Jing^1,2,*

¹Center for Translation Medicine Research on Sensory-Motor Diseases, Yan'an University, Yan'an 716000, China；²Key Laboratory of Yan'an Sports Rehabilitation Medicine, Yan'an 716000, China

Abstract

Endothelin-1 is a peptide derived from endothelial cells, consisting of 21 amino acid residues. In recent years, research has found that endothelin-1 not only plays a key role in vascular tone regulation but also participates in the occurrence and development of various types of pathological pain, including inflammatory pain, neuropathic pain, and cancer pain. Endothelin-1 binds to its receptors and activates multiple signaling pathways such as protein kinase C, calcium ion channels, and the phosphoinositide pathway, thereby influencing neuronal excitability and nociceptive information transmission. This article briefly reviews the current understanding of the mechanisms and potential roles of endothelin-1 in the development of pain, as well as commonly used endothelin-1 receptor antagonists, aiming to provide clues for better utilizing endothelin-1 and its receptors to alleviate and treat pathological pain.

Key words: Endothelin-1; pain; endothelin receptor

收稿日期：　　录用日期：

通讯作者：雷静　　E-mail:

DOI: 10.13294/j.aps.2025.0012

引用本文：

胡丛坤, 尤浩军, 雷静. 内皮素-1在疼痛中的作用及机制研究进展[J]. 生理学报 2025; 77 (1): 120-130.

HU Cong-Kun, YOU Hao-Jun, LEI Jing. Research progress on the role and mechanism of endothelin-1 in pain. Acta Physiol Sin 2025; 77 (1): 120-130 (in Chinese with English abstract).