Analgesic activity of acid-Sensing ion channel 3 (ASIC3) inhibitors: Sea anemones peptides Ugr9-1 and APETx2 versus low molecular weight compounds
Andreev Ya. A., Osmakov D. I., Koshelev S. G., Maleeva E. E., Logashina Yu. A., Palikov V. A., Palikova Y. A., Dyachenko I. A., Kozlov S. A.
Marine Drugs
Vol.16, Issue12, Num.500
Опубликовано: 2018
Тип ресурса: Статья
Аннотация:
Acid-sensing ion channel 3 (ASIC3) makes an important contribution to the development and maintenance of inflammatory and acid-induced pain. We compared different ASIC3 inhibitors (peptides from sea anemones (APETx2 and Ugr9-1) and nonpeptide molecules (sevanol and diclofenac)) in anti-inflammatory action and analgesic effects. All tested compounds had distinct effects on pH-induced ASIC3 current. APETx2 inhibited only transient current, whereas Ugr9-1 and sevanol decreased transient and sustained components of the current. The effect on mice was evaluated after administering an intramuscular injection in the acetic acid writhing pain model and the complete Freund’s adjuvant-induced thermal hyperalgesia/inflammation test. The bell-shaped dependence of the analgesic effect was observed for APETx2 in the acetic acid-induced writhing test, as well as for sevanol and peptide Ugr9-1 in the thermal hyperalgesia test. This dependence could be evidence of the nonspecific action of compounds in
Ключевые слова:
Acid-sensing ion channel; Animal models; APETx2; Pain relief; Toxin; Ugr 9-1
acetic acid; acid sensing ion channel blocking agent; apetx2; diclofenac; Freund adjuvant; lignan; sevanol; ugr9 1; unclassified drug; Accn3 protein, mouse; acetic acid; acid sensing ion channel; acid sensing ion channel blocking agent; analgesic agent; biological product; diclofenac; peptide; adult; analgesia; analgesic activity; animal cell; animal experiment; animal model; antiinflammatory activity; Article; comparative effectiveness; controlled study; dose response; drug efficacy; drug mechanism; drug potency; electrophysiology; hyperalgesia; in vitro study; in vivo study; male; mouse; nonhuman; open field test; paw edema; pH; thermal hyperalgesia; thermal hyperalgesia; visceral pain; writhing test; animal; chemically induced; disease model; drug effect; human; metabolism; nociception; pain; patch clamp technique; sea anemone; Xenopus laevis; Acetic Acid; Acid Sensing Ion Channel Blockers; Acid Sensing Ion Channels; Analgesics; Animals; Biological Products; Diclofenac; Disease Mode
Язык текста: Английский
ISSN: 1660-3397
Andreev Ya. A. Yaroslav Alekseevich 1979-
Osmakov D. I. Dmitrij Igorevich 1987-
Koshelev S. G.
Maleeva E. E.
Logashina Yu. A. Yuliya Aleksandrovna 1988-
Palikov V. A.
Palikova Y. A.
Dyachenko I. A.
Kozlov S. A.
Андреев Я. А. Ярослав Алексеевич 1979-
Осмаков Д. И. Дмитрий Игоревич 1987-
Кошелев С. Г.
Малеева Е. Е.
Логашина Ю. А. Юлия Александровна 1988-
Паликов В. А.
Паликова Y. А.
Дяченко И. А.
Козлов С. А.
Analgesic activity of acid-Sensing ion channel 3 (ASIC3) inhibitors: Sea anemones peptides Ugr9-1 and APETx2 versus low molecular weight compounds
Текст визуальный непосредственный
Marine Drugs
Molecular Diversity Preservation International
Vol.16, Issue12 Num.500
2018
Статья
Acid-sensing ion channel Animal models APETx2 Pain relief Toxin Ugr 9-1
acetic acid acid sensing ion channel blocking agent apetx2 diclofenac Freund adjuvant lignan sevanol ugr9 1 unclassified drug Accn3 protein, mouse acetic acid acid sensing ion channel acid sensing ion channel blocking agent analgesic agent biological product diclofenac peptide adult analgesia analgesic activity animal cell animal experiment animal model antiinflammatory activity Article comparative effectiveness controlled study dose response drug efficacy drug mechanism drug potency electrophysiology hyperalgesia in vitro study in vivo study male mouse nonhuman open field test paw edema pH thermal hyperalgesia thermal hyperalgesia visceral pain writhing test animal chemically induced disease model drug effect human metabolism nociception pain patch clamp technique sea anemone Xenopus laevis Acetic Acid Acid Sensing Ion Channel Blockers Acid Sensing Ion Channels Analgesics Animals Biological Products Diclofenac Disease Mode
Acid-sensing ion channel 3 (ASIC3) makes an important contribution to the development and maintenance of inflammatory and acid-induced pain. We compared different ASIC3 inhibitors (peptides from sea anemones (APETx2 and Ugr9-1) and nonpeptide molecules (sevanol and diclofenac)) in anti-inflammatory action and analgesic effects. All tested compounds had distinct effects on pH-induced ASIC3 current. APETx2 inhibited only transient current, whereas Ugr9-1 and sevanol decreased transient and sustained components of the current. The effect on mice was evaluated after administering an intramuscular injection in the acetic acid writhing pain model and the complete Freund’s adjuvant-induced thermal hyperalgesia/inflammation test. The bell-shaped dependence of the analgesic effect was observed for APETx2 in the acetic acid-induced writhing test, as well as for sevanol and peptide Ugr9-1 in the thermal hyperalgesia test. This dependence could be evidence of the nonspecific action of compounds in