action of clathrodin and analogues on voltage-gated sodium channels
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ID: 237285
2014
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Abstract
Clathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (NaV) channels. Since there is an urgent need for small molecule NaV channel ligands as novel therapeutics, clathrodin could represent an interesting lead compound. Therefore, clathrodin was reinvestigated for its potency and NaV channel subtype selectivity. Clathrodin and its synthetic analogues were subjected to screening on a broad range of NaV 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 NaV channels, hereby validating the pyrrole-2-aminoimidazole alkaloid structure as a core structure for future small molecule-based NaV channel modulators.
| Reference Key |
peigneur2014marineaction
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|---|---|
| Authors | ;Steve Peigneur;Aleš Žula;Nace Zidar;Fiona Chan-Porter;Robert Kirby;David Madge;Janez Ilaš;Danijel Kikelj;Jan Tytgat |
| Journal | jixie gongcheng xuebao/journal of mechanical engineering |
| Year | 2014 |
| DOI |
10.3390/md12042132
|
| URL | |
| Keywords | Keywords not found |
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