Clathrodin 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 represent an 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. © 2014 by the authors; licensee MDPI.
Peigneur, S., Žula, A., Zidar, N., Chan-Porter, F., Kirby, R., Madge, D., … Tytgat, J. (2014). Action of clathrodin and analogues on voltage-gated sodium channels. Marine Drugs, 12(4), 2132–2143. https://doi.org/10.3390/md12042132