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Journal of Pharmacology and Experimental Therapeutics

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Research ArticleNEUROPHARMACOLOGY

N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: II. In Vivo Characterization in Rat Models of Inflammatory and Neuropathic Pain

James D. Pomonis, James E. Harrison, Lilly Mark, David R. Bristol, Kenneth J. Valenzano and Katharine Walker
Journal of Pharmacology and Experimental Therapeutics July 2003, 306 (1) 387-393; DOI: https://doi.org/10.1124/jpet.102.046268
James D. Pomonis
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James E. Harrison
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Lilly Mark
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David R. Bristol
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Kenneth J. Valenzano
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Katharine Walker
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Abstract

The vanilloid receptor 1 (VR1) is a cation channel expressed predominantly by nociceptive sensory neurons and is activated by a wide array of pain-producing stimuli, including capsaicin, noxious heat, and low pH. Although the behavioral effects of injected capsaicin and the VR1 antagonist capsazepine have indicated a potential role for VR1 in the generation and maintenance of persistent pain states, species differences in the molecular pharmacology of VR1 and a limited number of selective ligands have made VR1 difficult to study in vivo. N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropryazine-1(2H)-carbox-amide (BCTC) is a recently described inhibitor of capsaicin- and acid-mediated currents at rat VR1. Here, we report the effects of BCTC on acute, inflammatory, and neuropathic pain in rats. Administration of BCTC (30 mg/kg p.o.) significantly reduced both mechanical and thermal hyperalgesia induced by intraplantar injection of 30 μg of capsaicin. In rats with Freund's complete adjuvantinduced inflammation, BCTC significantly reduced the accompanying thermal and mechanical hyperalgesia (3 mg/kg and 10 mg/kg p.o., respectively). BCTC also reduced mechanical hyperalgesia and tactile allodynia 2 weeks after partial sciatic nerve injury (10 and 30 mg/kg p.o.). BCTC did not affect motor performance on the rotarod after administration of doses up to 50 mg/kg p.o. These data suggest a role for VR1 in persistent and chronic pain arising from inflammation or nerve injury.

Footnotes

  • DOI: 10.1124/jpet.102.046268.

  • ABBREVIATIONS: VR1, vanilloid receptor 1; DRG, dorsal root ganglion; BCTC, N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carbox-amide; PWT, paw withdrawal threshold; PWL, paw withdrawal latency; FCA, Freund's complete adjuvant; PLSD, protected least significant difference; FW50, median fiber weight.

    • Received January 3, 2003.
    • Accepted April 3, 2003.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 306 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 306, Issue 1
1 Jul 2003
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Research ArticleNEUROPHARMACOLOGY

N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: II. In Vivo Characterization in Rat Models of Inflammatory and Neuropathic Pain

James D. Pomonis, James E. Harrison, Lilly Mark, David R. Bristol, Kenneth J. Valenzano and Katharine Walker
Journal of Pharmacology and Experimental Therapeutics July 1, 2003, 306 (1) 387-393; DOI: https://doi.org/10.1124/jpet.102.046268

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Research ArticleNEUROPHARMACOLOGY

N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: II. In Vivo Characterization in Rat Models of Inflammatory and Neuropathic Pain

James D. Pomonis, James E. Harrison, Lilly Mark, David R. Bristol, Kenneth J. Valenzano and Katharine Walker
Journal of Pharmacology and Experimental Therapeutics July 1, 2003, 306 (1) 387-393; DOI: https://doi.org/10.1124/jpet.102.046268
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