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Papers of the Week


Papers: 5 Oct 2024 - 11 Oct 2024


2024 Oct 03


Neuroscience


39368605

Negative allosteric modulator of Group Ⅰ mGluRs: Recent advances and therapeutic perspective for neuropathic pain.

Authors

Li JL, Zhu CH, Tian MM, Liu Y, Ma L, Tao LJ, Zheng P, Yu JQ, Liu N

Abstract

Neuropathic pain (NP) is a widespread public health problem that existing therapeutic treatments cannot manage adequately; therefore, novel treatment strategies are urgently required. G-protein-coupled receptors are important for intracellular signal transduction, and widely participate in physiological and pathological processes, including pain perception. Group I metabotropic glutamate receptors (mGluRs), including mGluR1 and mGluR5, are predominantly implicated in central sensitization, which can lead to hyperalgesia and allodynia. Many orthosteric site antagonists targeting Group I mGluRs have been found to alleviate NP, but their poor efficacy, low selectivity, and numerous side effects limit their development in NP treatment. Here we reviewed the advantages of Group I mGluRs negative allosteric modulators (NAMs) over orthosteric site antagonists based on allosteric modulation mechanism, and the challenges and opportunities of Group I mGluRs NAMs in NP treatment. This article aims to elucidate the advantages and future development potential of Group I mGluRs NAMs in the treatment of NP.