Disclosed herein is the discovery that an allosteric receptor site exists on the intracellular surface of Shaker class voltage-gated potassium ion channels that is distinct from the pore and is involved in regulating gating of the pore. A class of compounds has been identified that binds to this allosteric site and modulates the length of time the channel remains open. Based on these discoveries, novel methods of modulating the activity of Shaker class voltage-gated potassium ion channels and assays for determining which compounds are modulators of these ion channels are reported herein.
Pharmacological modulators of voltage-gated potassium ion channels