Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives

Ellen Gleeson, Janease Graham, Sandro Spiller, Irina Vetter, Richard Lewis, Peter Duggan, Kellie Tuck

    Research output: Contribution to journalArticle

    8 Citations (Scopus)

    Abstract

    A set of fluorophenoxyanilides, designed to be simplified analogues of previously reported ω-conotoxin GVIA mimetics, were prepared and tested for N-type calcium channel inhibition in a SH-SY5Y neuroblastoma FLIPR assay. N-type or Cav2.2 channel is a validated target for the treatment of refractory chronic pain. Despite being significantly less complex than the originally designed mimetics, up to a seven-fold improvement in activity was observed.

    Original languageEnglish
    Pages (from-to)2030-2045
    Number of pages16
    JournalMarine Drugs
    Volume13
    Issue number4
    DOIs
    Publication statusPublished - 1 Apr 2015

    Keywords

    • Cav2.2
    • Channel blocker
    • FLIPR
    • N-type calcium channel
    • Pain

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