Nipecotic acid directly activates GABA(A)-like ion channels

Richard Barrett-Jolley

    Research output: Contribution to journalArticle

    27 Citations (Scopus)


    The GABA-related compound nipecotic acid is commonly used to inhibit GABA uptake. This report shows that nipecotic acid can also directly activate GABA(A)-like chloride channels. When applied to outside-out patches of paraventricular neurones, nipecotic acid (1 mM) activated inward unitary currents (approximately 3 pA at a holding potential of -60 mV, E(Cl)+44 mV). The EC(50) for ion channel activation was approximately 300 microM, 3 fold greater than that found for GABA itself in this preparation. The nipecotic acid activated channels had similar conductance and kinetic properties to those of GABA activated channels in the same patches, reversed near E(Cl) and were inhibited by bicuculline (3 microM). This study indicates that for experiments in which relatively high concentrations of nipecotic acid are used, possible direct GABA(A) receptor agonist properties should be considered.
    Original languageEnglish
    Pages (from-to)673-678
    Number of pages6
    JournalBritish Journal of Pharmacology
    Issue number5
    Publication statusPublished - 1 Jul 2001


    Dive into the research topics of 'Nipecotic acid directly activates GABA(A)-like ion channels'. Together they form a unique fingerprint.

    Cite this