title: ÐÐµÑ Ð°Ð½Ð¸Ð·Ð¼Ñ Ð¸Ð½Ð³Ð¸Ð±Ð¸ÑÐ¾Ð²Ð°Ð½Ð¸Ñ AMPA ÑÐµÑÐµÐ¿ÑÐ¾ÑÐ¾Ð² Ð¿ÐµÐ½ÑÐ°Ð¼Ð¸Ð´Ð¸Ð½Ð¾Ð¼ Ð¸ Ð´Ð¸Ð¼Ð¸Ð½Ð°Ð·Ð¸Ð½Ð¾Ð¼
title: Ð²ÑÐ¿ÑÑÐºÐ½Ð°Ñ ÐºÐ²Ð°Ð»Ð¸ÑÐ¸ÐºÐ°ÑÐ¸Ð¾Ð½Ð½Ð°Ñ ÑÐ°Ð±Ð¾ÑÐ° Ð¼Ð°Ð³Ð¸ÑÑÑÐ°
titleType: Subtitle
title: Mechanisms of AMPA receptors inhibition by pentamidine and diminazene
Creators: name: ÐÐ¸Ð³ÑÐ»Ð¸Ð½, ÐÑÑÐµÐ½Ð¸Ð¹
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: 2021
Subjects: ÐÐ¸ÐºÑÐ¾Ð±Ð¸Ð¾Ð»Ð¾Ð³Ð¸Ñ
Ð¿ÐµÐ½ÑÐ°Ð¼Ð¸Ð´Ð¸Ð½
Ð´Ð¸Ð¼Ð¸Ð½Ð°Ð·Ð¸Ð½
AMPA ÑÐµÑÐµÐ¿ÑÐ¾ÑÑ
Ð¸Ð½Ð³Ð¸Ð±Ð¸ÑÐ¾Ð²Ð°Ð½Ð¸Ðµ
Ð¿Ð°ÑÑ-ÐºÐ»Ð°Ð¼Ð¿
Ð¼ÐµÑ Ð°Ð½Ð¸Ð·Ð¼Ñ

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description: Pentamidine and diminazene are compounds, which belong to aromatic diamidines, they are used in the clinic as drugs for diseases caused by microorganisms. This work demonstrates their concentration-dependent effect on AMPA-type glutamate receptors and that they are more active against calcium-permeable than against calcium-impermeable AMPA receptors, which is common feature of channel blockers. The inhibition by pentamidine and diminazene is non-competitive, and they are more effective in conditions favoring open AMPAR channels. The action of both compounds is voltage-dependent, and they can permeate through the channels into the cytoplasm. Such compounds may be useful for treating CNS pathologies involving glutamate excitotoxicity.