Next Article in Journal
Cladieunicellins M–Q, New Eunicellins from Cladiella sp.
Next Article in Special Issue
Synthesis and Biological Evaluation of Novel 3-Alkylpyridine Marine Alkaloid Analogs with Promising Anticancer Activity
Previous Article in Journal
Insights and Ideas Garnered from Marine Metabolites for Development of Dual-Function Acetylcholinesterase and Amyloid-β Aggregation Inhibitors
Previous Article in Special Issue
Two New Tryptamine Derivatives, Leptoclinidamide and (-)-Leptoclinidamine B, from an Indonesian Ascidian Leptoclinides dubius
Open AccessArticle

Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels

1
Catholic University Leuven (KULeuven), Toxicology and Pharmacology, Herestraat 49-Box 922, 3000 Leuven, Belgium
2
University of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, Slovenia
3
Xention Ltd., Iconix Park, London Road, Pampisford, Cambridge CB22 3EG, UK
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Mar. Drugs 2014, 12(4), 2132-2143; https://doi.org/10.3390/md12042132
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)
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
Show Figures

Figure 1

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.

Show more citation formats Show less citations formats

Article Access Map

1
Only visits after 24 November 2015 are recorded.
Back to TopTop