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Antipruritic effect of DA-5018, a capsaicin derivative, in mice

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Abstract

The antipruritic effect of DA-5018, a capsaicin derivative, was examined in mice. Male ICR mice were topically pretreated with Zostrix-HP (0.075% capsaicin cream), 0.1%, 0.3% DA-5018 cream or cream base (control) twice daily for 4 days. One hour after the last application, itch was induced either by compound 48/80 (50μg, s.c.) or leukotriene B4 (0.03 nmol, i.d.) injection into the rostral back of the animals, and the number of scratches made by the animals at the injection site was counted for 60 min post-injection. DA-5018 cream (both 0.1 and 0.3%) significantly inhibited compound 48/80-induced scratching when compared with the cream base control (p<0.01), while Zostrix-HP showed minimal inhibition of the scratching behavior. In leukotriene B4-induced itch model, Zostrix-HP and 0.3% DA-5018 cream significantly inhibited the scratching during the first 10-min period (p<0.01). The results suggest that DA-5018 cream can be used as an antipruritic agent and warrant clinical evaluation.

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References Cited

  • Andoh, T. and Kuraishi, Y., Intradermal leukotriene B4, but not prostaglandin E2, induces itch-associated responses in mice.Eur. J. Pharmacol., 353, 93–96 (1998).

    Article  PubMed  CAS  Google Scholar 

  • Andoh, T., Nagasawa, T. and Kuraishi, Y., Expression of tachykinin NK1 receptor mRNA in dorsal root ganglia of the mouse.Mol. Brain Res., 35, 329–332 (1996).

    Article  PubMed  CAS  Google Scholar 

  • Bae, E. J., Kim, S. H., Son, M. H., Kim, H. K., Shin, M. S., Kim, H. J. and Kim, W. B., Analgesic effects of DA-5018, a new capsaicin derivative, in hyperalgesia of experimental diabetic neuropathy.J. Kor. Diabetes Assoc., 21, 69–79 (1997).

    Google Scholar 

  • Basha, K. M. and Whitehouse, F. W., Capsaicin: a therapeutic option for painful diabetic neuropathy.Henry Ford Hosp. Med. J., 39, 138–140 (1991).

    PubMed  CAS  Google Scholar 

  • Bernstein, J. E., Parish, L. C., Rapaport, M., Rosenbaum, M. M. and Roenigk, H. H. Jr., Effects of topically applied capsaicin on moderate and severe psoriasis vulgaris.J. Am. Acad. Dermatol., 15, 504–507 (1986).

    PubMed  CAS  Google Scholar 

  • Bernstein, J. E., Swift, R. M., Soltani, K. and Lorincz, A. L., Antipruritic effect of an opiate antagonist, naloxone hydrochloride.J. Invest. Dermatol., 78, 82–83 (1982).

    Article  PubMed  CAS  Google Scholar 

  • Bjerring, P. and Arendt-Nielsen, L., Inhibition of histamine skin flare reaction following repeated topical applications of capsaicin.Allergy, 45, 121–125 (1990).

    Article  PubMed  CAS  Google Scholar 

  • Devillier, P., Drapeau, G., Renoux, M. and Regoli, D., Role of the N-terminal arginine in the histamine-releasing activity of substance P, bradykinin and related peptides.Eur. J. Pharmacol., 168, 53–69 (1989).

    Article  PubMed  CAS  Google Scholar 

  • Dunnett, C. W., A multiple comparison procedure for comparing several treatments with a control.J. Am. Stat. Assoc., 50, 1096–1121 (1955).

    Article  Google Scholar 

  • Ebertz, J. M., Hirshman, C. A., Kettelkamp, N. S., Uno, H. and Hanifin, J. M., Substance P-induced histamine release in human cutaneous mast cells.J. Invest. Dermatol., 88, 682–685 (1987).

    Article  PubMed  CAS  Google Scholar 

  • Ellis, C. N., Berberian, B., Sulica, V. I., Dodd, W. A., Jarratt, M. T., Katz, H. I., Prawer, S., Krueger, G., Rex, I. H. Jr. and Wolf, J. E., A double-blind evaluation of topical capsaicin in pruritic psoriasis.J. Am. Acad. Dermatol., 9, 438–442 (1993).

    Google Scholar 

  • Farber, E. M., Nickoloff, B. J., Recht, B. and Fraki, J. E., Stress, symmetry, and psoriasis: possible role of neuropeptides.J. Am. Acad. Dermatol., 14, 305–311 (1986).

    PubMed  CAS  Google Scholar 

  • Goodless, D. R. and Eaglstein, W. H., Branchioradial pruritus: treatment with topical capsaicin.J. Acad. Dermatol., 29, 783–784 (1993).

    CAS  Google Scholar 

  • Hagermark, O., Peripheral and central mediators of itch.Skin Pharmacol., 5, 1–8 (1992).

    PubMed  CAS  Google Scholar 

  • Hagermark, O., Hokfelt, T. and Pernow, B., Flare and itch induced by substance P in human skin.J. Invest. Dermatol., 71, 233–235 (1978).

    Article  PubMed  CAS  Google Scholar 

  • Handwerker, H. O., Pain and allodynia, itch and alloknesis: an alternative hypothesis.APS. J., 1, 135–139 (1992).

    Article  Google Scholar 

  • Kim, H. K., Bae, E. J., Shin, M. S., Son, M. H., Kim, S. H., Kim, W. B., Yang, J. and Kong, J. Y., Analgesic effects of DA-5018, a new capsaicin derivative after subcutaneous injection and topical application.J. Appl. Pharmacol., 5, 117–124 (1997).

    Google Scholar 

  • Kim, O. J., Kim, D. H., Kang, K. K., Baik, N. G., Kim, W. B. and Yang, J., Primary skin and eye irritation test of 0.3% DA-5018 cream, a new non-narcotic analgesic.J. Appl. Pharmacol., 4, 364–372 (1996).

    Google Scholar 

  • Kuraishi, Y., Nagasawa, T., Hayashi, K. and Satoh, M., Scratching behavior induced by pruritogenic but not algesiogenic agents in mice.Eur. J. Pharmacol., 275, 229–233 (1995).

    Article  PubMed  CAS  Google Scholar 

  • Lotti, T., Teofoli, P. and Tsampau, D., Treatment of aquagenic pruritus with topical capsaicin cream.J. Am. Acad. Dermatol., 30, 232–235 (1994).

    PubMed  CAS  Google Scholar 

  • Martin, H. A., Basbaum, A. I., Goetzl, E. J. and Levine, J. D., Leukotriene B4 decreases the mechanical and thermal thresolds of C-fiber nociceptors in the hairy skin of the rat.J. Neurophysiol., 60, 438–445 (1988).

    PubMed  CAS  Google Scholar 

  • Peikert, A., Hentrich, M. and Ochs, G., Topical 0.025% capsaicin in chronic post-herpetic neuralgia: efficacy, predictors of response and long-term course.J. Neurol., 238, 452–456 (1991).

    Article  PubMed  CAS  Google Scholar 

  • Rojavin, M. A., Cowan, A., Radzievsky, A. A. and Ziskin, M. C., Antipruritic effect of millimeter waves in mice: evidence for opioid involvement.Life Sci., 63, PL251-PL257 (1998).

    Article  PubMed  CAS  Google Scholar 

  • Scheffler, N. M., Sheitel, P. L. and Lipton, M. N., Treatment of painful diabetic neuropathy with capsaicin 0.075%.J. Am. Podiatr. Med. Assoc., 81, 288–293 (1991).

    PubMed  CAS  Google Scholar 

  • Schmelz, M., Schmidt, R., Bickel, A., Handwerker, H. O. and Torebjork, H. E., Specific C-receptors for itch in human skin.J. Neurosci., 17, 8003–8008 (1997).

    PubMed  CAS  Google Scholar 

  • Son, M. H., Bae, E. J., Kim, H. K., Shin, M. S., Kim, S. H., Kim, W. B., Yang, J. and Park, N. S., Analgesic effects of DA-5018, a new capsaicin derivative, against experimental acute pain.J. Appl. Pharmacol., 5, 67–73 (1997).

    Google Scholar 

  • von Frey, M., Zur physiologie der juckempfindung.Arch. Neerland Physiol., 7, 142–145 (1922).

    Google Scholar 

  • Wahlgren, C-F., Hagermark, O. and Bergstrom, R., Patients' perception of itch induced by histamine, compound 48/80 and wool fibres in atopic dermatitis.Acta. Derm. Venereol., 71, 488–494 (1990).

    Google Scholar 

  • Wallengren, J., Treatment of notalgia paresthetica with topical capsaicin.J. Am. Acad. Dermatol., 24, 286–288 (1991).

    Article  PubMed  CAS  Google Scholar 

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Correspondence to Byoung Ok Ahn.

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Kim, D.H., Ahn, B.O., Kim, S.H. et al. Antipruritic effect of DA-5018, a capsaicin derivative, in mice. Arch Pharm Res 22, 549–553 (1999). https://doi.org/10.1007/BF02975324

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