Potassium Channel - Blockers

Blockers

Potassium channel blockers, such as 4-aminopyridine and 3,4-diaminopyridine, have been investigated for the treatment of conditions such as multiple sclerosis.

These blockers work in a way to inhibit the flow of potassium ions through the KcsA channel. They either compete with potassium when binding to KcsA channel or they bind to the outside of the channel on an external binding site causing a conformational change, which closes the channel. An example of one of these competitors is quaternary ammonium ions, thought to be toxins that inhibit the binding of potassium. In a study it was found that Tyr82 residues provides a good external binding site for blockers, especially the quaternary ammonium ions.

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