Activation of G protein-coupled receptor 39 alleviates neuropathic pain and chronic inflammation

  • Impact factors: 3.6
  • Publication: JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
  • Author:Fang Cheng, Fengfeng Yan, Aixing Yang, Jing Liu, Jianxin Ma
  • DOI citation-doi:10.1002/jbt.23545
  • Date:2023-10-16

Neuropathic pain (NP) is mainly caused by lesions or diseases of the somatosensory nervous system and triggers severe physical burdens to patients. It is claimed that activated microglia-mediated neuroinflammation participates in the development of NP, which is regulated by p38 mitogen-activated protein kinase (MAPK)/nuclear factor-κappa B (NF-κB) p65 signaling. G protein-coupled receptor 39 (GPR39) is a trans-membrane protein involved in the activation of cellular transduction pathways, and TC-G 1008, a GPR39 agonist, is believed to have inhibitory effects on neuroinflammation. Our study will explore the possible alleviatory function of TC-G 1008 on NP in a rat model. GPR39 was found markedly downregulated in the spinal dorsal horn of chronic constriction injury (CCI)-stimulated rats. Rats were treated with CCI, followed by intranasal administration with 7.5 and 15 mg/kg TC-G 1008 at 1, 25, 49, and 73 h postmodeling, respectively. Drastically lowered values of paw withdrawal threshold and paw withdrawal latency, upregulated ionized calcium-binding adapter molecule 1, increased release of inflammatory cytokines, elevated spinal malondialdehyde levels, and reduced spinal glutathione peroxidase levels were observed in CCI-stimulated rats, all of which were markedly alleviated and rescued by TC-G 1008. Furthermore, the levels of p-p38/p38 and p‑NF‑κB p65 were found signally repressed in the spinal dorsal horn of CCI-stimulated rats, which was notably reversed by TC-G 1008. Collectively, TC-G 1008 markedly alleviated NP and neuroinflammation in CCI-treated rats. Our findings provide an attractive future direction for the treatment of NP.

Related Products

$400.00$500.00

$400.00$500.00

$400.00$500.00

$400.00$500.00

$400.00$500.00

$400.00$500.00

$400.00$500.00

EK1392

$350.00$450.00

EK1242

$350.00$450.00

EK1C01

$350.00$450.00

EK1341

$350.00$450.00

EK1334

$350.00$450.00

EK2295

$350.00$450.00

$350.00$450.00

EK2100

$350.00$450.00

EK1360

$350.00$450.00

Hot products

Hot citation