Molecular mechanism of action and safety of 5-(3-chlorophenyl)-4-hexyl-2,4-dihydro-3H-1,2,4-triazole-3-thione - a novel anticonvulsant drug candidate

نویسندگان

  • Barbara Kaproń
  • Jarogniew Łuszczki
  • Agata Paneth
  • Monika Wujec
  • Agata Siwek
  • Tadeusz Karcz
  • Barbara Mordyl
  • Monika Głuch-Lutwin
  • Anna Gryboś
  • Gabriel Nowak
  • Karolina Pająk
  • Krzysztof Jóźwiak
  • Adam Tomczykowski
  • Tomasz Plech
چکیده

Previously, it was found that 5-(3-chlorophenyl)-4-hexyl-2,4-dihydro-3H-1,2,4-triazole-3-thione (TP-315) effectively protects mice from maximal electroshock-induced seizures. The aim of this study was to determine possible interactions between TP-315 and different molecular targets, i.e. GABAA receptors, voltage-gated sodium channels, and human neuronal α7 and α4β2 nicotinic acetylcholine receptors. The influence of TP-315 on the viability of human hepatic HepG2 cells was also established using PrestoBlue and ToxiLight assays. It was found that the anticonvulsant activity of TP-315 results (at least partially) from its influence on voltage-gated sodium channels (VGSCs). Moreover, the title compound slightly affected the viability of human hepatic cells.

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عنوان ژورنال:

دوره 14  شماره 

صفحات  -

تاریخ انتشار 2017