23 April 2018
Int J Med Sci 2017; 14(8):741-749. doi:10.7150/ijms.20001
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
1. Department of Organic Chemistry, Medical University of Lublin, Chodzki 4A, 20-093 Lublin, Poland;
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.
Keywords: Sodium channels, [3H]-batrachotoxin, patch-clamp, cell viability assays.
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How to cite this article:
Kaproń B, Łuszczki J, Paneth A, Wujec M, Siwek A, Karcz T, Mordyl B, Głuch-Lutwin M, Gryboś A, Nowak G, Pająk K, Jóźwiak K, Tomczykowski A, Plech T. 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. Int J Med Sci 2017; 14(8):741-749. doi:10.7150/ijms.20001. Available from http://www.medsci.org/v14p0741.htm