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Pharmaceutical Chemistry Journal

, Volume 50, Issue 1, pp 19–23 | Cite as

Tropoxin – Drug for the Treatment of Migraine

  • T. S. Gan’shina
  • A. A. Gorbunov
  • A. V. Gnezdilova
  • A. I. Turilova
  • L. M. Kostochka
  • B. M. Pyatin
  • N. I. Avdyunina
  • L. N. Grushevskaya
  • R. S. Mirzoyan
Article
  • 80 Downloads

Anew antimigraine drug – Tropoxin (3-(3,4,5-trimethoxybenzoyloxyimino)-8-methyl-8-azabicyclo[1, 2, 3]octane hydrochloride) – was developed and was found to prevent or significantly weaken the constrictor reactions of cerebral arteries evoked by serotonin (5-HT) or the 5-HT2B/2C receptor agonist meta-chlorophenylpiperazine (m-CPP) in intact animals and in animals with ischemic brain damage. Tropoxin showed affinity for5-HT2 receptors in the brain and had antiaggregatory actions. It had no marked neurotropic properties and did not alter blood pressure responses to noradrenaline, acetylcholine, or histamine. Pilot clinical trials of Tropoxin provided evidence that it has high efficacy in the interictal treatment of frequent and severe migraine attacks.

Keywords

migraine Tropoxin tropan derivatives serotonin meta-chlorophenylpiperazine serotonin agonists cerebral circulation cerebral ischemia 

References

  1. 1.
    A. V. Amelin, Yu. D. Ignatov, and A. A. Skoromets, Migraine (Pathogenesis, Clinical Aspects, Treatment), St. Petersburg Medical Press, St. Petersburg (2001).Google Scholar
  2. 2.
    N. N. Yakhno, and D. R. Shtul’man, Diseases of the Nervous System. Handbook for Doctors [in Russian], Meditsina, Moscow (2003).Google Scholar
  3. 3.
    M. Schurks, R. Y. Zee, J. E. Buring, and T. Kurth, Cephalalgia, 30(4), 447 – 456 (2010); Doi:  10.1111/j.14682982.2009.PubMedPubMedCentralGoogle Scholar
  4. 4.
    P. M. Rist, J. E. Buring, C. S. Kase, et al., Circulation, 122(24), 2551 – 2557 (2010).CrossRefPubMedPubMedCentralGoogle Scholar
  5. 5.
    W. Dent, B. Stelzhammer, M. Meindl, et al., Headache, 51(10), 1483 – 1492 (2011); Doi:  10.1111/j.15264610.2011.CrossRefPubMedGoogle Scholar
  6. 6.
    A. Pezzini, E. Del Zotto, A. Giossi, et al., Stroke Res. Treatment, 9(2010); Doi: 10.4061/2011/304921.
  7. 7.
    D. Hoyer and G. Martin, Neuropharmacology, 36, 419 – 428 (1997).CrossRefPubMedGoogle Scholar
  8. 8.
    A. Panconesi and R. Sicuteri, Cephalalgia, 17, 3 – 14 (1997).CrossRefPubMedGoogle Scholar
  9. 9.
    P. J. Goadsby, Headache: The Journal of Head and Face Pain, 51(4), 650 – 653 (2011).CrossRefGoogle Scholar
  10. 10.
    V. Granados-Soto, C. F. Arguelles, H. I. Rocha-Gonzalez, et al., Neuroscience, 165, 561 – 568 (2010).CrossRefPubMedGoogle Scholar
  11. 11.
    S. J. Tepper, A. M. Rapoport, and F. D. Sheftell, Arch. Neurol., 59, 1084 – 1088 (2002).CrossRefPubMedGoogle Scholar
  12. 12.
    T. Muller and L. Lohse, Clin. Neuropharmacol., 34(6), 206 – 209 (2011).CrossRefPubMedGoogle Scholar
  13. 13.
    E. J. Mylecharane, J. Misbach, J. W. Duckworth, and J. W. Lance, Eur. J. Pharmacol., 48, 1 – 9 (1978).CrossRefPubMedGoogle Scholar
  14. 14.
    K. Schmuck, C. Ullmer, H. O. Kalkman, et al., Eur. J. Neurosci., 8(5), 959 – 967 (1996).CrossRefPubMedGoogle Scholar
  15. 15.
    G. Casucci, V. Villani, and F. Frediani, Neurol. Sci., 29, 123 – 126 (2008).CrossRefGoogle Scholar
  16. 16.
    J. A. Charles, Headache: The Journal of Head and Face Pain, 51(10), 1550 – 1551 (2011).CrossRefGoogle Scholar
  17. 17.
    A. Raizada, S. S. Vittala, M. Q. Najib, et al., Eur. J. Echocardiogr., 12(11), 880 (2011).CrossRefPubMedGoogle Scholar
  18. 18.
    R. S. Mirzoyan, S. B. Seredenin, T. S. Gan’shina, et al., Éksperim. Klin. Farmakol., 61(2), 28 – 31 (1998).Google Scholar
  19. 19.
    L. M. Kostochka, T. S. Gan’shina, R. S. Mirzoyan, and S. B. Seredenin, Khim.-Farm. Zh., 44, No. 9, 6 – 9 (2010); Pharm. Chem. J., 44(9), 472 – 475 (2010).Google Scholar
  20. 20.
    R. S. Mirzoyan, T. S. Gan’shina, D. V. Maslennikov, et al., BioMed. Res. Intern., Vol. 2014 (2014), Article ID 586501; http://dx.doi.org/ 10.1155/2014/586501.
  21. 21.
    R. C. Mirzoyan, M. B. Plotnikov, T. S. Gan’shina, et al., Handbook for Conducting Preclinical Studies of Drugs [in Russian], Grif i K, Moscow (2012), Part 1, pp. 480 – 487.Google Scholar
  22. 22.
    A. V. Topchyan, R. S. Mirzoyan, and M. G. Balasanyan, Éksperim. Klin. Farmakol., 59(5), 62 – 64 (1996).Google Scholar
  23. 23.
    A. A. Gorbunov, T. S. Gan’shina, and R. S. Mirzoyan, Éksperim. Klin. Farmakol., 73(9), 13 – 16 (2010).Google Scholar
  24. 24.
    A. Panconesi and R. Sicuteri, Cephalalgia, 17(1), 3 – 14 (1997).CrossRefPubMedGoogle Scholar
  25. 25.
    A. Yu. Sokolov, O. A. Lyubashina, and S. S. Panteleev, Neirokhimiya, 2, 104 – 112 (2011).Google Scholar
  26. 26.
    R. S. Mirzoyan, A. V. Topchyan, T. S. Gan’shina, and L. M. Kostochka, Éksperim. Klin. Farmakol., 63(3), 21 – 23 (2000).Google Scholar
  27. 27.
    T. S. Gan’shina, Éksperim. Klin. Farmakol., 66(3), 17 – 20 (2003).Google Scholar
  28. 28.
    M. D. Ferrari, M. Wilkinson, D. Hirt, et al., Pain, 45(3), 283 – 291 (1991).CrossRefPubMedGoogle Scholar
  29. 29.
    S. N. Kozhechkin, L. M. Kostochka, S. G Bezhanyan, et al., Éksperim. Klin. Farmakol., 68(4), 3 – 6 (2005).Google Scholar
  30. 30.
    T. M. Vasil’eva, G. N. Petrukhina, N. T. Miftakhova, et al., Éksperim. Klin. Farmakol., 68(3), 30 – 33 (2005).Google Scholar
  31. 31.
    A. V. Amelin, V. E. Ivanov, Yu. D. Ignatov, et al., Éksperim. Klin. Farmakol., 62(4), 14 – 17 (1999).Google Scholar

Copyright information

© Springer Science+Business Media New York 2016

Authors and Affiliations

  • T. S. Gan’shina
    • 1
  • A. A. Gorbunov
    • 1
  • A. V. Gnezdilova
    • 1
  • A. I. Turilova
    • 1
  • L. M. Kostochka
    • 1
  • B. M. Pyatin
    • 1
  • N. I. Avdyunina
    • 1
  • L. N. Grushevskaya
    • 1
  • R. S. Mirzoyan
    • 1
  1. 1.V. V. Zakusov Science Research Institute of PharmacologyMoscowRussia

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