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NMDA-Receptor Antagonists Reduce Skin Sensitivity to the TRPV1-Receptor Agonist Capsaicin

  • MOLECULAR-BIOLOGICAL PROBLEMS OF DRUG DESIGN AND MECHANISM OF DRUG ACTION
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Pharmaceutical Chemistry Journal Aims and scope

Glutamate receptors are widely represented in the central and peripheral nervous systems, which determines their involvement in central and peripheral nociception. In particular, NMDA receptors are localized at the dermal-epidermal junction. TRPV1 receptors in skin-innervating unmyelinated nerve fibers can functionally interact with NMDA receptors in the calcium/calmodulin-dependent protein kinase II and protein kinase C cascades. Herein, the effect of noncompetitive NMDA-receptor antagonists on peripheral skin sensitization caused by subcutaneous injection of the TRPV1-receptor agonist capsaicin was evaluated using different routes of administration. The high-affinity antagonist of NMDA receptors MK-801 and the low-affinity antagonist of NMDA receptors hemantane administered to mice by cutaneous application and systemic (intraperitoneal for hemantane and subcutaneous for MK-801) and subcutaneous injection in the metatarsal region reduced the duration of the response to subcutaneous injection of capsaicin solution in the metatarsal region.

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References

  1. Y. H. Jin, F. Yamaki, M. Takemura, et al., J. Pharmacol. Sci., 109(2), 233 – 241 (2009).

  2. D. P. Srebro, S. M. Vuckovic, K. R. Savic Vujovic, and M. S. Prostran, Tohoku J. Exp. Med., 234(4), 287 – 293 (2014).

    Article  CAS  Google Scholar 

  3. J. Lee, J. L. Saloman, G. Weiland, et al., Pain, 153(7), 1514 – 1524 (2012).

    Article  CAS  Google Scholar 

  4. M. Tominaga, M. J. Caterina, A. B. Malmberg, et al., Neuron, 21(3), 531 – 543 (1998).

    Article  CAS  Google Scholar 

  5. M. J. Caterina, A. Leffler, A. B. Malmberg, et al., Science, 288(5464), 306 – 313 (2000).

    Article  CAS  Google Scholar 

  6. R. E. Coggeshall and S. M. Carlton, J. Comp. Neurol., 391(1), 78 – 86 (1998).

  7. I. Kinkelin, E. B. Brocker, M. Koltzenburg, and S. M. Carlton, Neurosci. Lett., 283(2), 149 – 152 (2000).

    Article  CAS  Google Scholar 

  8. T. Sakurada, K. Katsumata, K. Tan-No, et al., Neuropharmacology, 31(12), 1279 – 1285 (1992).

  9. S. Nakamori, J. Takahashi, S. Hyuga, et al., J. Nat. Med., 71(1), 105 – 113 (2017).

    Article  CAS  Google Scholar 

  10. V. Tekus, K. Bolcskei, A. Kis-Varga, et al., Eur. J. Pharmacol., 641(2 – 3), 135 – 141 (2010).

  11. E. A. Ivanova, A. I. Matyushkin, E. V. Blynskaya, and T. A. Voronina, Khim. Farm. Zh., 52(8), 51 – 55 (2018); Pharm. Chem. J., 52(8), 740 – 743 (2018).

  12. C. R. McNamara, J. Mandel-Brehm, and D. M. Bautistaetal, Proc. Natl. Acad. Sci. USA, 104(33), 13525 – 13530 (2007).

  13. O. Gouin, K. L. Herondelle, N. Lebonvallet, et al., Protein Cell, 8(9), 644 – 661 (2017).

  14. A. Staruschenko, N. A. Jeske, and A. N. Akopian, J. Biol. Chem., 285(20), 15167 – 15177 (2010).

    Article  CAS  Google Scholar 

  15. Y. Kanai, T. Hara, and A. Imai, J. Pharm. Pharmacol., 58(4), 489 – 493 (2006).

    Article  CAS  Google Scholar 

Download references

Acknowledgments

The work was performed in the framework of a State Task on Topic No. 0521-2019-0007.

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Correspondence to E. A. Ivanova.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 55, No. 9, pp. 3 – 6, September, 2021.

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Ivanova, E.A., Matyushkin, A.I. & Voronina, T.A. NMDA-Receptor Antagonists Reduce Skin Sensitivity to the TRPV1-Receptor Agonist Capsaicin. Pharm Chem J 55, 857–859 (2021). https://doi.org/10.1007/s11094-021-02509-7

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  • DOI: https://doi.org/10.1007/s11094-021-02509-7

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