3-Alkyl- and 3-aryl-7H-furo[3,2-g]chromen-7-ones as blockers of the voltage-gated potassium channel Kv1.3.
3-Alkyl- and 3-aryl-7H-furo[3,2-g]chromen-7-ones were synthesised and studied for their effects on voltage-gated K+ and Na+ channels of the neuroblastoma cell-line N1E-115 and K+ channels of L-929 mouse-fibroblasts, stably transfected with mKv1.3. All furocoumarins tested showed Kv channel blocking activities, the most potent one in a half-blocking concentration of 0.7 microM.
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Pharmazeutisches Institut, Universität Kiel, Kiel, Germany.
Körner
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Hänsel
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D000818:Animals; D001932:Brain Neoplasms / Q000378:metabolism; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology*; D005347:Fibroblasts; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects; D051664:Kv1.3 Potassium Channel; D008564:Membrane Potentials / Q000187:drug effects; D051379:Mice; D009447:Neuroblastoma / Q000378:metabolism; D018408:Patch-Clamp Techniques; D026902:Potassium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D015221:Potassium Channels / Q000187:drug effects*; D024642:Potassium Channels, Voltage-Gated; D026941:Sodium Channel Blockers / Q000138:chemical synthesis / Q000494:pharmacology
D003374:Coumarins; C496973:KCNA3 protein, human; C496974:Kcna3 protein, mouse; D051664:Kv1.3 Potassium Channel; D026902:Potassium Channel Blockers; D015221:Potassium Channels; D024642:Potassium Channels, Voltage-Gated; D026941:Sodium Channel Blockers