{"refrec":{"BRefID":295560,"RR":"<b>Zidar, N.; Zula, A.; Tomašic, T.; Rogers, M.; Kirby, R.W.; Tytgat, J.; Peigneur, S.; Kikelj, D.; Ilas, J.; Masic, L.P.</b> (2017). Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels. <i>Eur. J. Med. Chem. 139</i>: 232-241. <a href=\"https://dx.doi.org/10.1016/j.ejmech.2017.08.015\" target=\"_blank\">https://dx.doi.org/10.1016/j.ejmech.2017.08.015</a>","BEntID":287647,"PublicFlag":1,"CheckedFlag":1,"wosflag":1,"vabbflag":0,"RefStringPartII":". <i>Eur. J. Med. Chem. 139</i>: 232-241. <a href=\"https://dx.doi.org/10.1016/j.ejmech.2017.08.015\" target=\"_blank\">https://dx.doi.org/10.1016/j.ejmech.2017.08.015</a>","DocTypID":8,"DocType":"Journal article","MarineFlag":1,"FreshFlag":0,"BrackishFlag":0,"TerrestrialFlag":0,"Authorstring":"Zidar, N.; Zula, A.; Tomašic, T.; Rogers, M.; Kirby, R.W.; Tytgat, J.; Peigneur, S.; Kikelj, D.; Ilas, J.; Masic, L.P.","OrigTitleTranslFlag":0,"Authorstringtrunc":"Zidar, N. <i>et al.</i>","Englishabstract":"We have prepared three alkaloids from the <i>Agelas</i> sponges, clathrodin, hymenidin and oroidin, and a series of their synthetic analogues, and evaluated their inhibitory effect against six isoforms of the K<sub>v</sub>1 subfamily of voltage-gated potassium channels, K<sub>v</sub>1.1-K<sub>v</sub>1.6, expressed in Chinese Hamster ovary (CHO) cells using automated patch clampelectrophysiology assay. The most potent inhibitor was the (E)-N-(3-(2-amino-1H-imidazol-4-yl)allyl)-4,5-dichloro-1H-pyrrole-2-carboxamide (6g) with IC<sub>50</sub> values between 1.4 and 6.1 μM against K<sub>v</sub>1.3, K<sub>v</sub>1.4, K<sub>v</sub>1.5 and K<sub>v</sub>1.6 channels. All compounds tested displayed selectivity against K<sub>v</sub>1.1 and K<sub>v</sub>1.2 channels. For confirmation of their activity and selectivity, compounds were additionally evaluated in the second independent system against K<sub>v</sub>1.1-K<sub>v</sub>1.6 and K<sub>v</sub>10.1 channels expressed in <i>Xenopus laevis</i> oocytes under voltage clamp conditions where IC<sub>50</sub> values against K<sub>v</sub>1.3-K<sub>v</sub>1.6 channels for the most active analogues (e.g. 6g) were lower than 1 μM. Because of the observed low sub-micromolar IC<sub>50</sub> values and fairly low molecular weights, the prepared compounds represent good starting points for further optimisation towards more potent and selective voltage-gated potassium channel inhibitors.","AbstractOtherLang":null,"BibLvlCode":"AS","StandardTitle":"Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels","OrigTitleLangCode":"en","OrigTitleLangCodeExtended":"eng","OrigTitleLangID":15,"DateLastModified":{"date":"2026-04-17 01:32:20.055033","timezone_type":1,"timezone":"+02:00"},"UserAccessRight":null,"UserAccID":null,"AuthorKeywords":"Voltage-gated potassium channel; K(v)1; Modulator; Inhibitor;Clathrodin; Oroidin; Hymenidin","OtherDescriptors":null,"Notes":null,"AnaPub":2017,"MonPub":null,"DateUpdate":"2022-05-23","DateCreate":"2018-05-15","SecASFANote":null,"ConfID":null,"PeerRev":1,"VlizCoreFlag":1,"WoScode":"WOS:000412788200019","VABBcode":null,"OpenAcc":0,"DOI":"10.1016/j.ejmech.2017.08.015"},"refs":null,"anarec":{"AnaID":295560,"PubliDate":2017,"Pagination":"232-241","XtraPublOfAnaID":null,"ISBN":null,"Volume":"139","Issue":null,"BRefMon":null,"BRefMonRR":null,"BRefXtra":null,"BRefXtraRR":null,"SerBRefID":258832,"SerRR":"European Journal of Medicinal Chemistry. 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