Abstract
A series of 4-aryl-3-aminoquinoline-2-one derivatives was synthesized and evaluated as activators of the cloned maxi-K channel mSlo (hSlo) expressed in Xenopus laevis oocytes using electrophysiological methods. A brain penetrable activator of maxi-K channels was identified and shown to be significantly active in the MCAO model of stroke.
MeSH terms
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Animals
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Brain / drug effects
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Clone Cells
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Disease Models, Animal
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Electrophysiology
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Large-Conductance Calcium-Activated Potassium Channels
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Male
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Membrane Potentials
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Neuroprotective Agents / blood
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Neuroprotective Agents / chemical synthesis
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Neuroprotective Agents / chemistry*
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Neuroprotective Agents / pharmacology
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Oocytes / metabolism
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Patch-Clamp Techniques
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Potassium Channels, Calcium-Activated / drug effects
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Potassium Channels, Calcium-Activated / metabolism*
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Quinolones / blood
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Quinolones / chemical synthesis
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Quinolones / chemistry*
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Quinolones / pharmacology
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Rats
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Stroke / complications
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Stroke / drug therapy
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Structure-Activity Relationship
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Xenopus laevis
Substances
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Large-Conductance Calcium-Activated Potassium Channels
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Neuroprotective Agents
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Potassium Channels, Calcium-Activated
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Quinolones