title: Ð¡ÑÑÑÐºÑÑÑÐ½Ð¾-ÑÑÐ½ÐºÑÐ¸Ð¾Ð½Ð°Ð»ÑÐ½Ð¾Ðµ Ð¸ÑÑÐ»ÐµÐ´Ð¾Ð²Ð°Ð½Ð¸Ðµ Ð´ÐµÐ¹ÑÑÐ²Ð¸Ñ Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÑ ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½Ð° Ð½Ð° AMPA-ÑÐµÑÐµÐ¿ÑÐ¾ÑÑ
title: Ð²ÑÐ¿ÑÑÐºÐ½Ð°Ñ ÐºÐ²Ð°Ð»Ð¸ÑÐ¸ÐºÐ°ÑÐ¸Ð¾Ð½Ð½Ð°Ñ ÑÐ°Ð±Ð¾ÑÐ° Ð±Ð°ÐºÐ°Ð»Ð°Ð²ÑÐ°
titleType: Subtitle
title: Structural and functional study of the phenytoin derivatives action AMPA-receptors
Creators: name: Ð¡ÐºÐ¾ÑÐ¾ÑÐ¾Ð´Ð¾Ð²Ð°, ÐÐ¾Ð»Ð¸Ð½Ð°
Publisher: name: Ð¡Ð°Ð½ÐºÑ-ÐÐµÑÐµÑÐ±ÑÑÐ³ÑÐºÐ¸Ð¹ Ð¿Ð¾Ð»Ð¸ÑÐµÑÐ½Ð¸ÑÐµÑÐºÐ¸Ð¹ ÑÐ½Ð¸Ð²ÐµÑÑÐ¸ÑÐµÑ ÐÐµÑÑÐ° ÐÐµÐ»Ð¸ÐºÐ¾Ð³Ð¾
Year: 2023
Subjects: ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½
Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÐµ ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½Ð°
Ð¿Ð°ÑÑ-ÐºÐ»Ð°Ð¼Ð¿
AMPA-ÑÐµÑÐµÐ¿ÑÐ¾ÑÑ
Ð¸Ð½Ð³Ð¸Ð±Ð¸ÑÐ¾Ð²Ð°Ð½Ð¸Ðµ
phenytoin
phenytoin derivatives
patch-clamp
ampa-receptors
inhibition

description: ÐÐ°Ð½Ð½Ð°Ñ ÑÐ°Ð±Ð¾ÑÐ° Ð¿Ð¾ÑÐ²ÑÑÐµÐ½Ð° Ð¸ÑÑÐ»ÐµÐ´Ð¾Ð²Ð°Ð½Ð¸Ñ Ð´ÐµÐ¹ÑÑÐ²Ð¸Ñ Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÑ ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½Ð° Ð½Ð° AMPA-ÑÐµÑÐµÐ¿ÑÐ¾ÑÑ. Ð¤ÐµÐ½Ð¸ÑÐ¾Ð¸Ð½ ÑÐ²Ð»ÑÐµÑÑÑ Ð¾ÑÐ½Ð¾Ð²Ð½ÑÐ¼ Ð¿ÑÐ¾ÑÐ¸Ð²Ð¾ÑÑÐ´Ð¾ÑÐ¾Ð¶Ð½ÑÐ¼ Ð¿ÑÐµÐ¿Ð°ÑÐ°ÑÐ¾Ð¼, ÐºÐ¾ÑÐ¾ÑÑÐ¹ Ð¾Ð±ÑÐ°ÑÐ¸Ð¼Ð¾ Ð¸Ð½Ð³Ð¸Ð±Ð¸ÑÑÐµÑ AMPA-ÑÐµÑÐµÐ¿ÑÐ¾ÑÑ Ñ IC50 250 Â± 60 Ð¼ÐºÐ Ð´Ð»Ñ CP-AMPAR Ð¸ IC50 30 Â± 4 Ð¼ÐºÐ Ð´Ð»Ñ CI-AMPAR. ÐÐ°Ð½Ð½ÑÐµ Ð±ÑÐ»Ð¸ Ð¿Ð¾Ð»ÑÑÐµÐ½Ñ Ð¼ÐµÑÐ¾Ð´Ð¾Ð¼ Ð¿Ð°ÑÑ-ÐºÐ»Ð°Ð¼Ð¿ Ð² ÐºÐ¾Ð½ÑÐ¸Ð³ÑÑÐ°ÑÐ¸Ð¸ Â«ÑÐµÐ»Ð°Ñ ÐºÐ»ÐµÑÐºÐ°Â». ÐÐ· ÑÑÐ´Ð° Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÑ ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½Ð° Ð½Ð°Ð¸Ð±Ð¾Ð»ÐµÐµ Ð°ÐºÑÐ¸Ð²Ð½ÑÐ¼Ð¸ Ð¾ÐºÐ°Ð·Ð°Ð»Ð¸ÑÑ 3,3-diphenyl-2,5-pyrrolidinedione Ð¸ 5-cyclohexyl-5-phenyl-2,4-imidazolidinedione, Ð¸Ð½Ð³Ð¸Ð±Ð¸ÑÑÑÑÐ¸Ðµ CI-AMPA ÑÐµÑÐµÐ¿ÑÐ¾ÑÑ Ñ IC50 26 Â± 2 Ð¼ÐºÐ Ð¸ Ñ IC50 11 Â± 1 Ð¼ÐºÐ, ÑÐ¾Ð¾ÑÐ²ÐµÑÑÑÐ²ÐµÐ½Ð½Ð¾. ÐÐ° Ð¾ÑÐ½Ð¾Ð²Ð°Ð½Ð¸Ð¸ Ð¿Ð¾Ð»ÑÑÐµÐ½Ð½ÑÑ Ð´Ð°Ð½Ð½ÑÑ Ð±ÑÐ»Ð° ÑÐ´ÐµÐ»Ð°Ð½Ð° Ð¾ÑÐµÐ½ÐºÐ° Ð·Ð½Ð°ÑÐ¸Ð¼Ð¾ÑÑÐ¸ ÑÑÑÑÐºÑÑÑÐ½ÑÑ ÑÐ»ÐµÐ¼ÐµÐ½ÑÐ¾Ð² Ð¼Ð¾Ð»ÐµÐºÑÐ»Ñ ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½Ð° Ð² ÐºÐ¾Ð½ÑÐµÐºÑÑÐµ ÐµÐ³Ð¾ Ð¸Ð½Ð³Ð¸Ð±Ð¸ÑÑÑÑÐµÐ³Ð¾ Ð´ÐµÐ¹ÑÑÐ²Ð¸Ñ. ÐÑÐ»Ð¸ Ð²ÑÐ´ÐµÐ»ÐµÐ½Ñ Ð½Ð°Ð¸Ð±Ð¾Ð»ÐµÐµ Ð·Ð½Ð°ÑÐ¸Ð¼ÑÐµ ÑÐ»ÐµÐ¼ÐµÐ½ÑÑ Ð¸ Ð±ÑÐ»Ð¾ Ð¾Ð¿ÑÐµÐ´ÐµÐ»ÐµÐ½Ð¾, ÑÑÐ¾ Ð½ÐµÐºÐ¾ÑÐ¾ÑÑÐµ Ð¸Ð· Ð½Ð¸Ñ Ð½Ðµ Ð¾ÐºÐ°Ð·ÑÐ²Ð°ÑÑ ÑÑÑÐµÑÑÐ²ÐµÐ½Ð½Ð¾Ð³Ð¾ Ð²Ð»Ð¸ÑÐ½Ð¸Ñ Ð½Ð° Ð¿ÑÐ¾ÑÐµÑÑ Ð¸Ð½Ð³Ð¸Ð±Ð¸ÑÐ¾Ð²Ð°Ð½Ð¸Ñ. Ð­ÑÐ¾ Ð¸ÑÑÐ»ÐµÐ´Ð¾Ð²Ð°Ð½Ð¸Ðµ Ð¼Ð¾Ð¶ÐµÑ Ð¿Ð¾Ð¼Ð¾ÑÑ ÑÐ»ÑÑÑÐ¸ÑÑ ÑÑÑÐµÐºÑÐ¸Ð²Ð½Ð¾ÑÑÑ Ð¸ Ð±ÐµÐ·Ð¾Ð¿Ð°ÑÐ½Ð¾ÑÑÑ Ð¿ÑÐ¸Ð¼ÐµÐ½ÐµÐ½Ð¸Ñ ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½Ð°, Ð° ÑÐ°ÐºÐ¶Ðµ Ð¼Ð¾Ð¶ÐµÑ Ð±ÑÑÑ Ð¸ÑÐ¿Ð¾Ð»ÑÐ·Ð¾Ð²Ð°Ð½Ð¾ Ð´Ð»Ñ ÑÐ°Ð·ÑÐ°Ð±Ð¾ÑÐºÐ¸ Ð½Ð¾Ð²ÑÑ Ð¿ÑÐ¾ÑÐ¸Ð²Ð¾ÑÐ¿Ð¸Ð»ÐµÐ¿ÑÐ¸ÑÐµÑÐºÐ¸Ñ Ð¿ÑÐµÐ¿Ð°ÑÐ°ÑÐ¾Ð², ÑÐ°Ð·ÑÐ°Ð±Ð¾ÑÐ°Ð½Ð½ÑÑ Ð½Ð° Ð¾ÑÐ½Ð¾Ð²Ðµ ÑÐµÐ½Ð¸ÑÐ¾Ð¸Ð½Ð°.
description: The given work is devoted to a study of the action of phenytoin derivatives on AMPA receptors. Phenytoin is a major anticonvulsant drug that reversibly inhibits AMPA receptors with an IC50 of 250 Â± 60 Î¼M for CP-AMPAR and an IC50 of 30 Â± 4 Î¼M for CI-AMPAR. The results were obtained by the patch-clamp method in a whole-cell configuration. Of the series of phenytoin derivatives, 3,3-diphenyl-2,5-pyrrolidinedione and 5-cyclohexyl-5-phenyl-2,4-imidazolidinedione were the most active, inhibiting CI-AMPA receptors with IC50 26 Â± 2 Î¼M and with IC50 11 Â± 1 Î¼M, respectively. On the basis of the data obtained, the significance of the structural elements of the phenytoin molecule in the context of its inhibitory action was evaluated. The most important elements were highlighted and it was determined that some of them do not have a significant effect on the inhibitory process. This study can help improve the efficacy and safety of phenytoin and can also be used to develop new antiepileptic drugs based on phenytoin.