phkineticaФармакокинетика и ФармакодинамикаPharmacokinetics and Pharmacodynamics2587-78362686-8830ООО «Издательство ОКИ»10.37489/2587-7836-2022-4-55-61phkinetica-344Research ArticleДОКЛИНИЧЕСКИЕ И КЛИНИЧЕСКИЕ ИССЛЕДОВАНИЯ БЕЗОПАСНОСТИ ЛЕКАРСТВЕННЫХ СРЕДСТВPRECLINICAL AND CLINICAL STUDIES OF DRUG SAFETYОценка фармакологической безопасности нового дипептидного миметика 2-й петли BDNF при совместном введении с этаноломAssessment of pharmacological safety of a new dipeptide mimetic of the 2nd loop of BDNF when co-administered with ethanolhttps://orcid.org/0000-0002-0463-2190НадороваА. В.NadorovaA. V.

Надорова Анна Владимировна, н. с. лаборатории фармакологической регуляции состояний зависимости

Москва

Nadorova Anna V., Research scientist, Laboratory of Pharmacological Regulation of Alcohol and Drug Addiction

Moscow

av-nadorova@mail.ruhttps://orcid.org/0000-0002-4290-4396ГригоревскихЕ. М.GrigorevskikhE. M.

Григоревских Екатерина Михайловна, н. с. лаборатории фармакологической регуляции состояний зависимости

Москва

Grigorevskikh Ekaterina M., Research scientist, laboratory of pharmacological regulation of alcohol and drug addiction

Moscow

https://orcid.org/0000-0001-9750-4157ТарасюкА. В.TarasiukA. V.

Тарасюк Алексей Валерьевич, н. с. лаборатории пептидных биорегуляторов отдела химии лекарственных средств

Москва

Tarasiuk Aleksey V., Research scientist, Laboratory of Peptide Bioregulators of Medicinal Chemistry Department

Moscow

https://orcid.org/0000-0002-7608-7419СазоноваН. М.SazonovaN. M.

Сазонова Нелля Михайловна, к. х. н., с. н. с. лаборатории пептидных биорегуляторов отдела химии лекарственных средств

Москва

Sazonova Nellya M., PhD, Cand. Chemistry Sci., senior research scientist, laboratory of peptide bioregulators of medicinal chemistry department

Moscow

https://orcid.org/0000-0002-9847-8058КоликЛ. Г.KolikL. G.

Колик Лариса Геннадьевна, д. б. н., профессор РАН, руководитель лаборатории фармакологической регуляции состояний зависимости

Москва

Kolik Larisa G., Dr. Sci. (Biol.), professor RAS, Head laboratory of pharmacological regulation of alcohol and drug addiction

SPIN code: 9126-6922

Moscow

lgkolik@mail.ruФГБНУ «НИИ фармакологии имени В.В. Закусова»РоссияFSBI «Zakusov Institute of Pharmacology»Russian Federation202218012023045561Copyright © Надорова А.В., Григоревских Е.М., Тарасюк А.В., Сазонова Н.М., Колик Л.Г., 20232023Надорова А.В., Григоревских Е.М., Тарасюк А.В., Сазонова Н.М., Колик Л.Г.Nadorova A.V., Grigorevskikh E.M., Tarasiuk A.V., Sazonova N.M., Kolik L.G.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.pharmacokinetica.ru/jour/article/view/344

Для оценки фармакологической безопасности дипептидного миметика 2-й петли BDNF (соединение ГТС-201) при совместном введении с этанолом изучено его влияние на изменение двигательной активности, вызываемое этанолом при остром и субхроническом введении у мышей C57Bl/6 и DBA/2. Установлено, что ГТС-201 в дозе 5,0 мг/кг, в/б, не влияя на спонтанную двигательную активность per se, при предварительном однократном введении препятствовал развитию седативной реакции, вызываемой этанолом (2,0 г/кг, в/б) у мышей C57Bl/6. При субхроническом введении ГТС-201 лишён психостимулирующего действия и влияния на формирование поведенческой сенсибилизации, индуцированной этанолом, у мышей DBA/2. Полученные данные свидетельствуют об отсутствии в фармакологическом профиле ГТС-201 психостимулирующего компонента и синергизма при использовании с этанолом в низкой дозе.

To assess the pharmacological safety of the dipeptide mimetic of the 2nd loop of BDNF (compound GTS-201) when co-administered with ethanol, its effect on the alteration in motor activity induced by ethanol during acute and subchronic administration in mice C57Bl/6 and DBA/2 was studied. It was found that GTS-201 at a dose of 5.0 mg / kg, i.p., without affecting spontaneous motor activity per se, after a preliminary acute administration prevented the development of a sedative reaction caused by ethanol (2.0 g/ kg, i.p.) in C57Bl/6 mice. After subchronic administration, GTS-201 is devoid of psychostimulant effect and impact on the formation of ethanol-induced behavioral sensitization in DBA/2 mice. The data obtained indicate the absence of a psychostimulant component and synergism in the pharmacological profile of GTS-201 when used with ethanol at low dose.

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The authors declare that there are no conflicts of interest present.