Гипогликемическая Активность Новых Агонистов Рецепторов Глюкагоноподобного Пептида-1

Тюренков, Иван Николаевич; Куркин, Д. В.; Бакулин, Дмитрий Александрович; Волотова, Е. В.; Абросимова, Елизавета Евгеньевна; Бородкина, Людмила Евгеньевна

doi:10.30906/0869-2092-2020-83-2-27-33

Cited by 2 publications

(2 citation statements)

References 4 publications

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“…Индукция секреции ГПП-1 свободными жирными кислотами (СЖК или Free Fatty Acids -FFA) сильно зависит от концентрации Ca 2+ в цитозоле. СЖК увеличивают секрецию ГПП-1, стимулируя приток внеклеточного Ca 2+ через каналы Ca 2+ на поверхности клетки [26,35,36].…”

Section: влияние липидов на секрецию гпп-1unclassified

“…Эти рецепторы (GPR40, GPR41, GPR43, GPR119 и GPR120) были открыты при реализации проекта «геном человека», а в последующем была установлена их значимая роль в регуляции биосинтеза инкретинов и углеводном обмене. Активация рецепторов GPR40 помимо инкретинопосредованных эффектов оказывает гепато-и нейропротекторное действие, GPR41 и GPR43 влияет на метаболизм лептина, дифференцировку адипоцитов нервную и иммунную системы [35,36], метаболические и плейотропные эффекты агонистов GPR119 [35,37] и GPR120 активно изучаются [26,27,30]. Агонисты ГПП-1Р последовательно увеличивают своё присутствие на российском фармацевтическом рынке.…”

Section: стимуляторы секреции эндогенного гпп-1unclassified

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Physiology and pharmacology of glucagon-like peptide-1 receptor

Kurkin,

Bakulin,

Morkovin

et al. 2024

Farm. farmakol. (Pâtigorsk)

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Modern approaches to the treatment of type 2 diabetes mellitus (T2DM) are aimed not only at glycemic control, but also at reducing cardiovascular risks. The increasing prevalence of the disease and the need for effective treatment options highlight the importance of glucagon-like peptide-1 (GLP-1) receptor agonists in the pharmacotherapy structure.The aim of the work was to review the literature regarding the physiology of GLP-1 and the therapeutic potential and development trends of its agonists.Materials and methods. The search for the review materials was carried out using the abstract databases of PubMed, Google Scholar and e-Library. The search was carried out for publications from 2000 to 2023, using the following keywords: “GLP-1”; “GLP-1R agonists”; “GIP”; “exenatide”; “liraglutide”; “dulaglutide”; “semaglutide”; “lixisenatide”; “albiglutide”; “taspoglutide” taking into account various spellings.Results. The interaction of almost all food components with enteroendocrine cells of the intestine leads to the secretion of incretins (primarily GLP-1) into the blood, triggering a complex of physiological reactions aimed primarily at the rapid utilization of incoming glucose (regulation of insulin and glucagon secretion), as well as the central regulation of dietary behavior (slowing gastric emptying and the formation of a feeling of satiety). A wide distribution of the GLP-1 receptor in various tissues and organs, its connection with intracellular signaling cascades aimed at launching energy-consuming remodeling (recovery) processes in endothelial cells, heart, neurons, beta cells, etc., is the basis for a wide range of pleiotropic effects of GLP-1 unrelated to its hypoglycemic effect. The discovery of synthetic GLP-1 receptor agonists with a long period of action has made it possible not only to therapeutically influence various parts of carbohydrate metabolism disorders, but also to increase the functional reserves of the target diabetes organs, reducing the risk of developing complications of the disease. Incretin-like drugs are well tolerated, with nausea being the most common side effect. The factors limiting a wider use of the drugs include their high cost and the preferred form of a subcutaneous solution. The current research is focused on the development of long-acting, oral, dual and triple agonists, fixed-dose combinations, and small molecule drugs.Conclusion. GLP-1 receptor agonists are a class of effective and safe drugs for the treatment of diabetes and obesity, which is rapidly developing in the most advanced areas of pharmacy. A further development of this group and the solution of the identified problems will open up new opportunities for the treatment of diabetes and its complications.

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Section: влияние липидов на секрецию гпп-1unclassified

Section: стимуляторы секреции эндогенного гпп-1unclassified

Physiology and pharmacology of glucagon-like peptide-1 receptor

Kurkin,

Bakulin,

Morkovin

et al. 2024

Farm. farmakol. (Pâtigorsk)

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Aspects of effect of novel compound exhibiting hypoglycemic activity on female rat reproduction processes

Bugaeva,

Denisova,

Tyurenkov

et al. 2023

Journal of Volgograd State Medical University

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In experiments, in female rats, the novel substance dipiarone with hypoglycemic activity when administered intragastrically at doses of 0.5 mg/kg and 100 mg/kg from 6 to 16 days of gestation did not have a damaging effect on the processes of organo- and fetogenesis and did not contribute to the occurrence of deformities and abnormalities in the development of fetuses recorded in the antenatal and postnatal period of their development. Intragastric administration of dipiarone to rats at a dose of 100 mg/kg from 6 days of pregnancy until delivery showed that the formation of physical development of rat offspring in the postnatal period corresponds to the control parameters, while they had an increase in the rate of body weight gain, ahead of the time of formation of sensory-motor reflexes, activation of motor and emotional behavior.

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Гипогликемическая Активность Новых Агонистов Рецепторов Глюкагоноподобного Пептида-1

Cited by 2 publications

References 4 publications

Physiology and pharmacology of glucagon-like peptide-1 receptor

Physiology and pharmacology of glucagon-like peptide-1 receptor

Aspects of effect of novel compound exhibiting hypoglycemic activity on female rat reproduction processes

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