Analgesic Activity of a Polypeptide Modulator of TRPV1 Receptors
D’yachenko I. A., Belous G. I., Skobtsova L. A., Zharmukhamedova T. Y., Palikov V. A., Palikova Y. A., D’yachenko E. V., Kalabina E. A., Rudenko V. B., Andreev Ya. A., Logashina Yu. A., Kozlov S. A., Yavorskii A. N., Murashev A. N.
Pharmaceutical Chemistry Journal
Vol.52, Issue3, P. 213-215
Опубликовано: 2018
Тип ресурса: Статья
DOI:10.1007/s11094-018-1793-6
Аннотация:
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. © 2018, Springer Science+Business Media, LLC, part of Springer Nature.
Ключевые слова:
analgesics; polypeptide modulator; TRPV1 receptors
analgesic agent; polypeptide; polypeptide aphc2; unclassified drug; vanilloid receptor 1; vanilloid receptor 1 antagonist; activated partial thromboplastin time; analgesic activity; animal experiment; animal model; Article; body temperature; comparative study; controlled study; heart rate; heat sensitivity; hemodynamics; hemostasis; hot plate test; locomotion; male; mouse; musculoskeletal system; nonhuman; prothrombin time; thermal stimulation
Язык текста: Английский
ISSN: 1573-9031
D’yachenko I. A.
Belous G. I.
Skobtsova L. A.
Zharmukhamedova T. Y.
Palikov V. A.
Palikova Y. A.
D’yachenko E. V.
Kalabina E. A.
Rudenko V. B.
Andreev Ya. A. Yaroslav Alekseevich 1979-
Logashina Yu. A. Yuliya Aleksandrovna 1988-
Kozlov S. A.
Yavorskii A. N.
Murashev A. N.
Д’яченко И. А.
Белоус Г. И.
Скобцова Л. А.
Жармухамедова Т. Y.
Паликов В. А.
Паликова Y. А.
Д’яченко Е. В.
Калабина Е. А.
Руденко В. Б.
Андреев Я. А. Ярослав Алексеевич 1979-
Логашина Ю. А. Юлия Александровна 1988-
Козлов С. А.
Яворскии А. Н.
Мурашев А. Н.
Analgesic Activity of a Polypeptide Modulator of TRPV1 Receptors
Текст визуальный непосредственный
Pharmaceutical Chemistry Journal
Springer New York Consultants Bureau
Vol.52, Issue3 P. 213-215
2018
Статья
analgesics polypeptide modulator TRPV1 receptors
analgesic agent polypeptide polypeptide aphc2 unclassified drug vanilloid receptor 1 vanilloid receptor 1 antagonist activated partial thromboplastin time analgesic activity animal experiment animal model Article body temperature comparative study controlled study heart rate heat sensitivity hemodynamics hemostasis hot plate test locomotion male mouse musculoskeletal system nonhuman prothrombin time thermal stimulation
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. © 2018, Springer Science+Business Media, LLC, part of Springer Nature.