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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

Received: 　　Accepted:

Corresponding author: 雷静　　E-mail:

DOI: 10.13294/j.aps.2025.0012

Citing This Article：

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).