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Mar. Drugs 2014, 12(4), 2132-2143; doi:10.3390/md12042132
Article

Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels

1,†
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 and 1,*
Received: 3 January 2014; in revised form: 21 February 2014 / Accepted: 25 March 2014 / Published: 4 April 2014
(This article belongs to the Special Issue Alkaloid Analogs)
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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.
Keywords: clathrodin; oroidin; hymenidin; voltage-gated sodium channels; sodium channel modulator; sponge clathrodin; oroidin; hymenidin; voltage-gated sodium channels; sodium channel modulator; sponge
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Peigneur, S.; Žula, A.; Zidar, N.; Chan-Porter, F.; Kirby, R.; Madge, D.; Ilaš, J.; Kikelj, D.; Tytgat, J. Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels. Mar. Drugs 2014, 12, 2132-2143.

AMA Style

Peigneur S, Žula A, Zidar N, Chan-Porter F, Kirby R, Madge D, Ilaš J, Kikelj D, Tytgat J. Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels. Marine Drugs. 2014; 12(4):2132-2143.

Chicago/Turabian Style

Peigneur, Steve; Žula, Aleš; Zidar, Nace; Chan-Porter, Fiona; Kirby, Robert; Madge, David; Ilaš, Janez; Kikelj, Danijel; Tytgat, Jan. 2014. "Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels." Mar. Drugs 12, no. 4: 2132-2143.



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