Mechanisms of G Protein-Coupled Receptors (GPCRs) in Inflammatory Pain and Their Therapeutic Targets

² Department of Anesthesiology, First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310003, Zhejiang, China; Department of Anesthesiology, Yinzhou No. 2 Hospital, Ningbo 315100, Zhejiang, China,

BAS 2025 , 3(2), 14–19; https://doi.org/10.26689/bas.v3i2.10139

© 2025 by the Authors. Licensee Whioce Publishing, Singapore. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution 4.0 International License ( https://creativecommons.org/licenses/by/4.0/ )

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Abstract

Inflammatory pain is a common and complex clinical symptom closely associated with many chronic inflammatory diseases, and its treatment has always faced significant challenges. As a receptor family playing a key role in cell signaling, G protein-coupled receptors (GPCRs) play an important role in the occurrence, development, and regulation of inflammatory pain. GPCRs not only regulate inflammatory responses and pain sensitivity through cell membrane signaling pathways but also interact complexly with ion channels, immune cells, and metabolites, affecting the dynamic balance of the neuro-inflammatory-immune network. Studies have shown that specific GPCR subtypes (such as Mrgpr, GPR37, etc.) play a unique role in inflammatory pain perception and inflammation resolution, providing targets for the development of new analgesic drugs. In addition, biased ligands of GPCRs and their endosome targeting effects open up new directions for reducing drug side effects and improving efficacy. This article systematically summarizes the biological functions of GPCRs in inflammatory pain, potential drug targets, and future research directions.

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