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|Action of Clathrodin and analogues on voltage-gated sodium channels|Peigneur, S.; Zula, A; Zidar, N; Chan-Porter, F; Kirby, R; Madge, D; Ilas, J; Kikelj, D; Tytgat, J. (2014). Action of Clathrodin and analogues on voltage-gated sodium channels. Mar. Drugs 12(4): 2132-2143. dx.doi.org/10.3390/md12042132
In: Marine Drugs. Molecular Diversity Preservation International (MDPI): Basel. ISSN 1660-3397; e-ISSN 1660-3397, meer
clathrodin; oroidin; hymenidin; voltage-gated sodium channels; sodiumchannel modulator; sponge
|Auteurs|| || Top |
- Peigneur, S.
- Zula, A
- Zidar, N.
- Chan-Porter, F
- Kirby, R
- Madge, D
- Ilas, J.
- Kikelj, D.
- Tytgat, J.
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.