Action of clathrodin and analogues on voltage-gated sodium channels

Peigneur, Steve (author), Žula, Aleš (author), Zidar, Nace (author), Chan-Porter, Fiona (author), Kirby, Robert (author), Madge, David J. (author), Ilaš, Janez (author), Kikelj, Danijel (author), Tytgat, Jan (author)

Clathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (Na$_V$) channels. Since there is an urgent need for small molecule Na$_V$ channel ligands as novel therapeutics, clathrodin could representan interesting lead compound. Therefore, clathrodin was reinvestigated for its potency and Na$_V$ channel subtype selectivity. Clathrodin and its synthetic analogues were subjected to screening on a broad range of Na$_V$ 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 Na$_V$ channels, hereby validating the pyrrole-2-aminoimidazole alkaloid structure as a core structure for future small molecule-based Na$_V$ channel modulators.

• Language: English
• Keywords: clathrodin, oroidin, hymenidin, voltage-gated sodium channels, sodium channel modulator, sponge
• Work type: Article
• Typology: 1.01 - Original Scientific Article
• Organization: FFA - Faculty of Pharmacy
• Publication status: Published
• Publication version: Version of Record
• Year: 2014
• Number of pages: Str. 2132-2143
• Numbering: Vol. 12, iss. 4
• PID: 20.500.12556/RUL-129226
• UDC: 615.454+615.21
• ISSN on article: 1660-3397
• DOI: 10.3390/md12042132
• COBISS.SI-ID: 3629681
• Publication date in RUL: 30.08.2021

Record is a part of a journal

• Title: Marine drugs
• Shortened title: Mar. drugs
• Publisher: MDPI
• ISSN: 1660-3397
• COBISS.SI-ID: 23578841

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