Docking analysis of 1,4-benzodiazepines with alpha-1 adrenergic receptor and phosphodiesterase 4
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Дата
2024
Науковий керівник
Укладач
Редактор
Назва журналу
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E-ISSN
Назва тому
Видавець
Одеський національний університет імені І. І. Мечникова
Анотація
«Propoxazepam», an innovative drug created by scientist of the O. V. Bogatsky Physical-Chemical Institute of the National Academy of Sciences of Ukraine and CAR «INTERCHIM», has an original pharmacodynamic profile, and can inhibit both acute and chronic pain, as well as have anti-inflammatory and anticonvulsant effects. Propoxazepam's analgesic effect is mediated by its dopaminergic system, NMDA receptors, and alpha-1 adrenoceptors. Midazolam, diazepam, and lorazepam, which are benzodiazepines, have been proposed to act as positive allosteric modulators (PAMs) for α1‐ ARs. In contrast, multiple benzodiazepines had a positive impact on phenylephrine's stimulation of a cAMP response element pathway through α1A‐ and α1B‐ ARs; from the literature it appears that this was caused by off-target inhibition of phosphodiesterase, which are known targets of diazepam.
Опис
Ключові слова
«Propoxazepam», 1,4-benzodiazepines, alpha-1 adrenergic receptor
Бібліографічний опис
Akisheva A. S. Docking analysis of 1,4-benzodiazepines with alpha-1 adrenergic receptor and phosphodiesterase 4 / A. S. Akisheva, V. B. Larionov, J. A. Makarenko et al. // Сучасна фармація: реалії сьогодення та перспективи розвитку [Електронний ресурс] : тези допов. Всеукр. наук.-практ. конф. з міжнар. участю (Одеса, 9–12 квіт. 2024 р.). – Одеса : Одес. нац. ун-т ім. І. І. Мечникова, 2024. – С. 116–119.