Large conductance Ca(2+)-activated K(+) channel (BKCa) activating properties of a series of novel N-arylbenzamides: Channel subunit dependent effects

Large conductance calcium activated potassium channels (BKCa) are fundamental in the control of cellular excitability. Thus, compounds that activate BKCa channels could provide potential therapies in the treatment of pathologies of the cardiovascular and central nervous system. A series of novel N-a...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2013-07, Vol.21 (14), p.4186-4191
Main Authors: Kirby, R W, Martelli, A, Calderone, V, McKay, N G, Lawson, K
Format: Article
Language:English
Subjects:
Benzamides - pharmacology
Benzimidazoles - pharmacology
HEK293 Cells
Humans
Large-Conductance Calcium-Activated Potassium Channels - drug effects
Large-Conductance Calcium-Activated Potassium Channels - metabolism
Molecular Structure
Protein Subunits - metabolism
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Summary:Large conductance calcium activated potassium channels (BKCa) are fundamental in the control of cellular excitability. Thus, compounds that activate BKCa channels could provide potential therapies in the treatment of pathologies of the cardiovascular and central nervous system. A series of novel N-arylbenzamide compounds, and the reference compound NS1619, were evaluated for BKCa channel opener properties in Human Embryonic Kidney (HEK293) cells expressing the human BKCa channel α-subunit alone or α+β1-subunit complex. Channel activity was determined using a non-radioactive Rb(+) efflux assay to construct concentration effect curves for each compound. All N-arylbenzamide compounds and NS1619 evoked significant (p
ISSN:1464-3391
DOI:10.1016/j.bmc.2013.05.003