Regulatory mechanisms of vanilloid receptor on pain signaling

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We cloned cDNA encording vanilloid receptor (TRPV1) from porcine and human spinal cord cDNA library. We established in vitro assay system for monitoring vanilloid receptor activities. Heterologous expressed TRPV1 receptors are activated by not only capsaicin, heat and protons, but also regulated by extracellular sodium ions. Hyperalgesia induced by inflammatory mediators, such as serotonin and histamine is due to a hyper-activation of TRPV1 using heterologous expression system and cultured sensory neurons. We found that mustard oil and methylsalicylate act as TRPV1 agonist and the latter produces marked desensitization of TRPV1 resulting in anti-nociception for capsaicin-induced pain. These data suggest that TRPV1 is important target molecule especially for inflammation-induced hyperalgesia.