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Analgesic Activity of a Polypeptide Modulator of TRPV1 Receptors

The activity of APHC2, a new polypeptide modulator of TRPV1 receptors that was isolated from Heteractis crispa, is studied. It was established that APHC2 possessed analgesic properties, did not disturb normal locomotor activity, and did not change body temperature and hemostasis of experimental animals. These attributes could be of great practical value for designing a new generation of efficacious analgesics. A brief increase of heart rate was observed during studies of the hemodynamic activity. Further investigation of the binding specifics of this polypeptide with TRPV1 receptors could open approaches to discovering other antagonists of these receptors.

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Acknowledgments

The work was performed using equipment at the IBC CUC with support from the RF Ministry of Education and Science, contract identifier RFMEFI62117X0018. The work was supported by the RFBR (Grant No. 15-04-04666), the RAS Presidium Basic Research Program “Molecular and Cellular Biology,” and a grant of the RF President for state support of leading scientific schools NSh-7676.2016.4.

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Correspondence to I. A. D’yachenko.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 52, No. 3, pp. 25 – 27, March, 2018.

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D’yachenko, I.A., Belous, G.I., Skobtsova, L.A. et al. Analgesic Activity of a Polypeptide Modulator of TRPV1 Receptors. Pharm Chem J 52, 213–215 (2018). https://doi.org/10.1007/s11094-018-1793-6

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  • DOI: https://doi.org/10.1007/s11094-018-1793-6

Keywords

  • polypeptide modulator
  • TRPV1 receptors
  • analgesics