Elsevier

Neuroscience Letters

Volume 228, Issue 1, 30 May 1997, Pages 29-32
Neuroscience Letters

Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia

https://doi.org/10.1016/S0304-3940(97)00358-3Get rights and content

Abstract

Vanilloid receptors are activated by capsaicin, the pungent ingredient in hot pepper. They are also specifically and competitively inhibited by capsazepine (CPZ). To determine whether CPZ is specific to vanilloid receptors, its effects were tested on the currents evoked by nicotine in rat trigeminal ganglia. We found that 10 μM CPZ, a concentration frequently used to inhibit capsaicin's physiological responses attributed to capsaicin, reversibly inhibits (40%) the magnitude of the currents activated by 100 μM nicotine. We conclude that 10 μM capsazepine can alter the effects of channels other than those activated by capsaicin, and thus caution must be used in attributing all the CPZ-sensitive physiological effects to those only produced by blocking of vanilloid receptors.

Section snippets

Acknowledgements

This work was supported by NIH grant DC-01065 and a grant from the Philip Morris Corporation.

References (25)

  • S. Bevan et al.

    Capsazepine: a competitive antagonist of the sensory neurone excitant capsaicin

    Br. J. Pharmacol.

    (1992)
  • M. Duner-Engstrom et al.

    Autonomic mechanisms underlying capsaicin induced oral sensations and salivation in man

    J. Physiol.

    (1996)
  • Cited by (162)

    • Lipid-dependent sequential allosteric activation of heat-sensing TRPV1 channels by anchor-stereoselective “hot” vanilloid compounds and analogs

      2021, Biochemistry and Biophysics Reports
      Citation Excerpt :

      The IC50 is ranged from nanomolar to low micromolar. Although it can also activate the noxious chemical sensor TRPA1 [12], or inhibit the cold-activated TRPM8 channel [13], voltage-activated calcium channels [14], and nicotinic acetylcholine receptors [15], capsazepine is mainly used as a tool to study the TRPV1 channel. The 3D cryo-EM structures have confirmed the overall similarity of TRPV1 to other tetrameric cation channels (Fig. 1) [3,4,16].

    • Comparison of joint degeneration and pain in male and female mice in DMM model of osteoarthritis

      2021, Osteoarthritis and Cartilage
      Citation Excerpt :

      Our study has limitations. Although CPZ has shown efficacy in inflammatory and neuropathic pain as well as OA animal models, it is known as a non-selective antagonist, which could exhibit off-target effects, thus, there is the possibility that CPZ modulated DMM-induced pain through receptors other than TRPV147–50. The dose of CPZ was rather low, and it is possible that sex difference in analgesic difference is attenuated at higher doses than those used in our study.

    • 3.20 - Oral Chemesthesis and Taste

      2020, The Senses: A Comprehensive Reference: Volume 1-7, Second Edition
    View all citing articles on Scopus
    View full text