Abstract
The ion channel TRPV1, which is one of the most important integrators of pain and inflammatory stimuli, is considered a promising therapeutic target in the treatment of pain conditions. In this work, we performed a comparative study of the analgesic effect in the “hot plate” test of recombinant analogues of Kunitz-type peptides from the sea anemone Heteractis crispa venom: APHC1—modulator of TRPV1 and HCRG21—a full blocker of TRPV1. As a result of biological tests, it was shown that the full blocker HCRG21, despite the higher value of 50% effective concentration of TRPV1 inhibition, had an equal analgesic ability with the APHC1 upon intramuscular administration and retained it for 13 h of observation. The analgesic effect of APHC1 at a dose of 0.1 mg/kg when administered intramuscularly developed very quickly in 5 min but lasted 3 h. The differences in the pharmacodynamic profile of the peptides are in good agreement with different mechanisms of binding to TRPV1.
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Funding
This work was supported by the Russian Science Foundation (project no. 19-74-20088). The study was performed using the equipment of the core facility of the Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry, which was supported by the Ministry of Education and Science of the Russian Federation (agreement identifier RFMEFI62117X0018).
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Translated by M. Batrukova
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Sintsova, O.V., Palikov, V.A., Palikova, Y.A. et al. Peptide Blocker of Ion Channel TRPV1 Exhibits a Long Analgesic Effect in the Heat Stimulation Model. Dokl Biochem Biophys 493, 215–217 (2020). https://doi.org/10.1134/S1607672920030096
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DOI: https://doi.org/10.1134/S1607672920030096