Sigma-1 Receptor Antagonist BD1047 Reduces Allodynia and Spinal ERK Phosphorylation Following Chronic Compression of Dorsal Root Ganglion in Rats.
10.4196/kjpp.2010.14.6.359
- Author:
Ji Seon SON
1
;
Young Bae KWON
Author Information
1. Department of Anesthesiology and Pain Medicine, Institute for Medical Science, Chonbuk National University Medical School, Jeonju 561-180, Korea.
- Publication Type:Original Article
- Keywords:
Allodynia;
Dorsal root ganglion;
Extracellular signal-regulated kinase;
Neuropathic pain;
Sigma-1 receptor
- MeSH:
Amines;
Animals;
Cold Temperature;
Constriction, Pathologic;
Cyclohexanecarboxylic Acids;
Ethylenediamines;
gamma-Aminobutyric Acid;
Ganglia, Spinal;
Humans;
Hyperalgesia;
Lumbar Vertebrae;
Neuralgia;
Phosphorylation;
Phosphotransferases;
Rats;
Receptors, sigma;
Salicylamides;
Spinal Nerve Roots;
Stainless Steel
- From:The Korean Journal of Physiology and Pharmacology
2010;14(6):359-364
- CountryRepublic of Korea
- Language:English
-
Abstract:
Many therapeutic roles have been proposed for sigma-1 receptor (Sig-1R), but the involvement of Sig-1R in neuropathic pain has currently not been well explored. The present study aimed to evaluate the anti-nociceptive effect of Sig-1R antagonist (BD1047) in a rat model of chronic compression of the dorsal root ganglion (CCD), which is a model of human foraminal stenosis and radicular pain. When stainless steel rods were inserted into the intervertebral foramen of lumbar vertebrae 4 and 5, the CCD developed reliable mechanical (from 3 day) and cold allodynia (from 1 day) as compared with the sham operation group. The spinal expressions of Sig-1R and phosphorylation of extracellular signal-regulated kinase (pERK) were significantly increased from day 3 to day 14 after CCD surgery, as is consistent with the manifestation of allodynia. The BD 1047 (10, 30, 100 mg/kg) administered on postoperative days 0~5 dose-dependently suppressed both the induction of allodynia and the elevation of the spinal pERK expression in a manner comparable with that of gabapentin (100 mg/kg). At 7 days post-CCD surgery, BD1047 (10, 30, 100 mg/kg) administration also produced anti-nociceptive effects on the mechanical and cold allodynia similar with those of gabapentin (100 mg/kg). Therefore, this data suggested that Sig-1R may play an important role in both the development and maintenance of CCD-induced neuropathy.
