Peptide Blocker of Ion Channel TRPV1 Exhibits a Long Analgesic Effect in the Heat Stimulation Model
| Autor: | Irina Gladkikh, V. A. Palikov, Oksana Sintsova, Igor A. Dyachenko, Margarita Monastyrnaya, A. A. Klimovich, Y. A. Palikova, Kozlovskaya Emma P, Ya. A. Andreev, Elena Leychenko, Sergey A. Kozlov |
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| Rok vydání: | 2019 |
| Předmět: |
Hot Temperature
Analgesic Biophysics TRPV1 Pain Sequence Homology TRPV Cation Channels Peptide Stimulation Venom Pharmacology Biochemistry Injections Intramuscular Mice Cnidarian Venoms Animals Amino Acid Sequence Ion channel chemistry.chemical_classification Analgesics Mice Inbred ICR General Chemistry General Medicine Disease Models Animal Nociception Sea Anemones chemistry Pharmacodynamics Peptides |
| Zdroj: | Doklady. Biochemistry and biophysics. 493(1) |
| ISSN: | 1608-3091 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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