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Duration and Dose–Response Relationship of the Analgesic Action of the Tetrapeptide H-Tyr-D-Arg-Phe-Gly-NH2 (Taphalgin), a Synthetic Derivative of Dermorphine, in Comparison with Morphine Hydrochloride

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The effect of the tetrapeptide H-Tyr-D-Arg-Phe-Gly-NH2 (Taphalgin), a synthetic derivative of dermorphine, was evaluated in the tail-flick test in mice after a single subcutaneous (s.c.) injection. Taphalgin significantly prolongs the tail-flick latency when administered in the dose range 0.01 – 5 mg/kg. The analgesic effect of a single s.c. injection of Taphalgin at 1 mg/kg exceeds the effect of morphine hydrochloride at the same dose. The effect of Taphalgin at 0.5 mg/kg is comparable to that of morphine hydrochloride at 1 mg/kg. The magnitude and duration of the analgesic effect grow as the dose of Taphalgin increases from 0.5 to 1.5 and 4.5 mg/kg. The maximum 4-h duration of the analgesic effect is observed at doses of 1.5 and 4.5 mg/kg.

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Acknowledgments

The research was supported by PVP Labs Pte. Ltd.

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Authors and Affiliations

  1. Research Zakusov Institute of Pharmacology, 8 Baltiiskaya St., Moscow, 125315, Russia

    E. A. Ivanova & T. A. Voronina

  2. M. V. Lomonosov Moscow State University, 27/1 Lomonosovskii Prosp., Moscow, 119192, Russia

    N. V. Korobov

  3. N. N. Blokhin National Medical Research Center of Oncology, Ministry of Health of Russia, 24 Kashirskoe Shosse, Moscow, 115478, Russia

    V. S. Kosorukov

Authors
  1. E. A. Ivanova
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  2. T. A. Voronina
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  3. N. V. Korobov
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  4. V. S. Kosorukov
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Correspondence to V. S. Kosorukov.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 56, No. 9, pp. 8 – 12, September, 2022.

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Ivanova, E.A., Voronina, T.A., Korobov, N.V. et al. Duration and Dose–Response Relationship of the Analgesic Action of the Tetrapeptide H-Tyr-D-Arg-Phe-Gly-NH2 (Taphalgin), a Synthetic Derivative of Dermorphine, in Comparison with Morphine Hydrochloride. Pharm Chem J 56, 1164–1168 (2022). https://doi.org/10.1007/s11094-022-02771-3

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  • DOI: https://doi.org/10.1007/s11094-022-02771-3

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