Opening of large-conductance calcium-activated potassium channels by the substituted benzimidazolone NS004

M. C. McKay, S. I. Dworetzky, N. A. Meanwell, S. P. Olesen, P. H. Reinhart, I. B. Levitan, John Adelman, V. K. Gribkoff

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Abstract

1. We used electrophysiological techniques to examine the effects of 5- trifluoromethyl-1-(5-chloro-2-hydroxyphenyl)-1,3-dihydro-2H-benzimidazole-2- one (NS004) on large-conductance calcium-activated potassium (BK) channels. 2. We used recordings from excised membrane patches (cell-attached and inside-out single-channel configurations) and whole-cell patch-clamp recordings to examine the effects of NS004 on single BK channels and whole- cell outward currents, respectively, in rat GH3 clonal pituitary tumor cells. We also tested NS004 on voltage-clamped BK channels isolated from rat brain plasma membrane preparations and reconstituted into planar lipid bilayers. Finally, we used two-electrode voltage-clamp techniques to study the effects of NS004 on currents expressed in Xenopus laevis oocytes by the recently described Slo BK clone from Drosophila. 3. In GH3 cells and in Xenopus oocytes expressing the Slo gene product NS004 produced an increase in an iberiotoxin- or tetraethylammonium-sensitive whole-cell outward current, respectively. NS004 produced a significant increase in the activity of single GH3 cell BK channels and rat brain BK channels reconstituted into planar lipid bilayers. In both systems this was characterized by an increase in channel mean open time, a decrease in interburst interval, and an apparent increase in channel voltage/calcium sensitivity. 4. These data indicate that NS004 could be useful for investigating the biophysical and molecular properties of BK channels and for determining the functional consequences of the opening of BK channels.

Original languageEnglish (US)
Pages (from-to)1873-1882
Number of pages10
JournalJournal of Neurophysiology
Volume71
Issue number5
StatePublished - 1994
Externally publishedYes

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Large-Conductance Calcium-Activated Potassium Channels
Lipid Bilayers
Oocytes
Cell Membrane
Tetraethylammonium
benzimidazolone
Xenopus laevis
Brain
Pituitary Neoplasms
Patch-Clamp Techniques
Calcium Channels
Xenopus
Drosophila
Electrodes
Clone Cells

ASJC Scopus subject areas

  • Physiology
  • Neuroscience(all)

Cite this

McKay, M. C., Dworetzky, S. I., Meanwell, N. A., Olesen, S. P., Reinhart, P. H., Levitan, I. B., ... Gribkoff, V. K. (1994). Opening of large-conductance calcium-activated potassium channels by the substituted benzimidazolone NS004. Journal of Neurophysiology, 71(5), 1873-1882.

Opening of large-conductance calcium-activated potassium channels by the substituted benzimidazolone NS004. / McKay, M. C.; Dworetzky, S. I.; Meanwell, N. A.; Olesen, S. P.; Reinhart, P. H.; Levitan, I. B.; Adelman, John; Gribkoff, V. K.

In: Journal of Neurophysiology, Vol. 71, No. 5, 1994, p. 1873-1882.

Research output: Contribution to journalArticle

McKay, MC, Dworetzky, SI, Meanwell, NA, Olesen, SP, Reinhart, PH, Levitan, IB, Adelman, J & Gribkoff, VK 1994, 'Opening of large-conductance calcium-activated potassium channels by the substituted benzimidazolone NS004', Journal of Neurophysiology, vol. 71, no. 5, pp. 1873-1882.
McKay MC, Dworetzky SI, Meanwell NA, Olesen SP, Reinhart PH, Levitan IB et al. Opening of large-conductance calcium-activated potassium channels by the substituted benzimidazolone NS004. Journal of Neurophysiology. 1994;71(5):1873-1882.
McKay, M. C. ; Dworetzky, S. I. ; Meanwell, N. A. ; Olesen, S. P. ; Reinhart, P. H. ; Levitan, I. B. ; Adelman, John ; Gribkoff, V. K. / Opening of large-conductance calcium-activated potassium channels by the substituted benzimidazolone NS004. In: Journal of Neurophysiology. 1994 ; Vol. 71, No. 5. pp. 1873-1882.
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AU - Dworetzky, S. I.

AU - Meanwell, N. A.

AU - Olesen, S. P.

AU - Reinhart, P. H.

AU - Levitan, I. B.

AU - Adelman, John

AU - Gribkoff, V. K.

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