News Release

Allosteric modulation of G protein-coupled receptors as a novel therapeutic strategy in neuropathic pain

Peer-Reviewed Publication

Compuscript Ltd


This new article publication from Acta Pharmaceutica Sinica B, discusses allosteric modulation of G protein-coupled receptors as a novel therapeutic strategy in neuropathic pain.


Neuropathic pain is a debilitating pathological condition that presents significant therapeutic challenges in clinical practice.


Unfortunately, current pharmacological treatments for neuropathic pain lack clinical efficacy and often lead to harmful adverse reactions. As G protein-coupled receptors (GPCRs) are widely distributed throughout the body, including the pain transmission pathway and descending inhibition pathway, the development of novel neuropathic pain treatments based on GPCRs allosteric modulation theory is gaining momentum.


Extensive research has shown that allosteric modulators targeting GPCRs on the pain pathway can effectively alleviate symptoms of neuropathic pain while reducing or eliminating adverse effects.


This article aims to provide a comprehensive summary of the progress made in GPCRs allosteric modulators in the treatment of neuropathic pain, and discuss the potential benefits and adverse factors of this treatment. The development of biased agonists of GPCRs are also covered, and based on important examples of biased agonist development in recent years, universal strategies for designing structure-based biased agonists are described.


It is foreseeable that, with the continuous improvement of GPCRs allosteric modulation and biased agonist theory, effective GPCRs allosteric drugs will eventually be available for the treatment of neuropathic pain with acceptable safety.


Keywords: Neuropathic pain, Allosteric modulators, G protein-coupled receptors, Analgesia

Graphical Abstract: available at

The allosteric modulation based on four key GPCRs (μ-OR, A1R, mGluRs and CBRs) shows promise as a therapeutic strategy for neuropathic pain. Allosteric modulators effectively mitigate non-specific side effects by modulating the affinity or efficacy of the orthosteric ligands, or through biased signaling effects.

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The Journal of the Institute of Materia Medica, the Chinese Academy of Medical Sciences and the Chinese Pharmaceutical Association.

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CiteScore: 19.4

Impact Factor: 14.5

JIF without self-citation: 13.7

ISSN 2211-3835

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Chunhao Zhu, Xiaobing Lan, Zhiqiang Wei, Jianqiang Yu, Jian Zhang, Allosteric modulation of G protein-coupled receptors as a novel therapeutic strategy in neuropathic pain, Acta Pharmaceutica Sinica B, Volume 14, Issue 1, 2024, Pages 67-86, ISSN 2211-3835,

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