Action of clathrodin and analogues on voltage-gated sodium channelsPeigneur, Steve (Avtor) Žula, Aleš (Avtor) Zidar, Nace (Avtor) Chan-Porter, Fiona (Avtor) Kirby, Robert (Avtor) Madge, David J. (Avtor) Ilaš, Janez (Avtor) Kikelj, Danijel (Avtor) Tytgat, Jan (Avtor) clathrodinoroidinhymenidinvoltage-gated sodium channelssodium channel modulatorspongeClathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (Na$_V$) channels. Since there is an urgent need for small molecule Na$_V$ channel ligands as novel therapeutics, clathrodin could representan interesting lead compound. Therefore, clathrodin was reinvestigated for its potency and Na$_V$ channel subtype selectivity. Clathrodin and its synthetic analogues were subjected to screening on a broad range of Na$_V$ channel isoforms, both in voltage clamp and patch clamp conditions. Even though clathrodin was not found to exert any activity, some analogues were capable of modulating the Na$_V$ channels, hereby validating the pyrrole-2-aminoimidazole alkaloid structure as a core structure for future small molecule-based Na$_V$ channel modulators.20142021-08-30 14:23:18Članek v reviji129226sl