Negative allosteric modulator of Group â
mGluRs: Recent advances and therapeutic perspective for neuropathic pain.
Neuroscience
; 2024 Oct 03.
Article
in En
| MEDLINE
| ID: mdl-39368605
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
Neuroscience
Year:
2024
Document type:
Article
Affiliation country:
China
Country of publication:
United States