Abstract
The novel K+ channel blocker 6,10-diaza-3(1,3)8,(1,4)-dibenzena-1,5(1,4)-diquinolinacy clodecaphane (UCL 1684) has been tested for its ability to inhibit Ca2+ -activated K+ currents in cultured rat chromaffin cells. Low nanomolar concentrations of UCL 1684 produced a rapid and reversible inhibition of the slow, apamin-sensitive, tail current activated by a depolarizing voltage command. This compound also inhibited the muscarine activated outward current with an IC50 of 6 nM. These results confirm UCL 1684 to be the most potent non-peptidic blocker of the apamin-sensitive Ca2+ -activated K+ channel so far described.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenal Glands / cytology
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Adrenal Glands / drug effects
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Adrenal Glands / physiology
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Alkanes / chemistry
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Alkanes / pharmacology*
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Animals
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Apamin / pharmacology
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Calcium / physiology
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Chromaffin Cells / cytology
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Chromaffin Cells / drug effects
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Chromaffin Cells / physiology
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Dose-Response Relationship, Drug
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Gallamine Triethiodide / pharmacology
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Male
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Membrane Potentials / drug effects
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Muscarine / pharmacology
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Muscarinic Agonists / pharmacology
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Neuromuscular Nondepolarizing Agents / pharmacology
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Patch-Clamp Techniques
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Potassium Channel Blockers*
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Potassium Channels / physiology
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Quinolinium Compounds / chemistry
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Quinolinium Compounds / pharmacology*
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Rats
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Rats, Sprague-Dawley
Substances
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6,10-diaza-3(1,3),8(1,4)dibenzena-1,5(1,4)diquinolinacyclodecaphane
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Alkanes
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Muscarinic Agonists
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Neuromuscular Nondepolarizing Agents
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Potassium Channel Blockers
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Potassium Channels
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Quinolinium Compounds
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Apamin
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Muscarine
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Gallamine Triethiodide
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Calcium