The Korean Journal of Physiology and Pharmacology

The Korean Society of Pharmacology (대한약리학회)
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The Antinociceptive Effect of Sigma-1 Receptor Antagonist, BD1047, in a Capsaicin Induced Headache Model in Rats

  • Kwon, Young-Bae (Department of Pharmacology, College of Medicine, Chonbuk National University) ;
  • Jeong, Young-Chan (Department of Pharmacology, College of Medicine, Chonbuk National University) ;
  • Kwon, Jung-Kee (Department of Laboratory Animal Medicine, College of Veterinary Medicine, Chonbuk National University) ;
  • Son, Ji-Seon (Department of Anesthesiology and Pain Medicine, College of Medicine, Chonbuk National University) ;
  • Kim, Kee-Won (Department of Pharmacology, College of Medicine, Chonbuk National University)
  • Published : 2009.12.31
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Abstract

Intracranial headaches, including migraines, are mediated by nociceptive activation of the trigeminal nucleus caudalis (TNC), but the precise mechanisms are poorly understood. We previously demonstrated that selective blockage of spinal sigma-1 receptors (Sig-1R) produces a prominent antinociceptive effect in several types of pain models. This study evaluates whether the Sig-1R antagonist (BD1047) has an antinociceptive effect on capsaicin (a potent C-fiber activator) induced headache models in rats. Intracisternal infusion of capsaicin evoked pain behavior (face grooming), which was significantly attenuated by BD1047 pretreatment. BD1047 consistently reduced capsaicin-induced Fos-like immunoreactivity (Fos-LI), a neuronal activator, in the TNC in a dose-dependent manner. Moreover, capsaicininduced phosphorylation of N-methyl-D-aspartate receptor subunit 1 was reversed by BD1047 pretreatment in the TNC. These results indicate that the Sig-1R antagonist has an inhibitory effect on nociceptive activation of the TNC in the capsaicin-induced headache animal model.

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References

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