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Mar. Drugs 2014, 12(4), 2132-2143;

Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels

Catholic University Leuven (KULeuven), Toxicology and Pharmacology, Herestraat 49-Box 922, 3000 Leuven, Belgium
University of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, Slovenia
Xention Ltd., Iconix Park, London Road, Pampisford, Cambridge CB22 3EG, UK
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 3 January 2014 / Revised: 21 February 2014 / Accepted: 25 March 2014 / Published: 4 April 2014
(This article belongs to the Special Issue Alkaloid Analogs)
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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. View Full-Text
Keywords: clathrodin; oroidin; hymenidin; voltage-gated sodium channels; sodium channel modulator; sponge clathrodin; oroidin; hymenidin; voltage-gated sodium channels; sodium channel modulator; sponge

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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.

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