Mechanism of Inhibition of Voltage-Gated Potassium Channels by Guanidine Compounds

Voltage-Gated Potassium Channels

Physiol. Soc.. ESSN: 1548-9221. Visit our website at http://www.the-aps.org/. American Physiological Society, 9650 Rockville Pike, Bethesda MD 20814-3991. ©2012 Int. Union Physiol. Sci./Am. the physiological developments. It is published bimonthly in February, April, June, August, October, and December by (formerly published as News in Physiological Science) publishes brief review articles on m...

Mechanism of Electromechanical Coupling in Voltage-Gated Potassium Channels

Voltage-gated ion channels play a central role in the generation of action potentials in the nervous system. They are selective for one type of ion - sodium, calcium, or potassium. Voltage-gated ion channels are composed of a central pore that allows ions to pass through the membrane and four peripheral voltage sensing domains that respond to changes in the membrane potential. Upon depolarizati...

Elucidating the molecular basis of action of a classic drug: guanidine compounds as inhibitors of voltage-gated potassium channels.

Guanidine and its alkyl analogs stimulate the neuromuscular junction presynaptically by inhibiting voltage-gated potassium (Kv) channels, leading to enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases myasthenic syndrome of Lambert-Eaton and botulism. The therapeutic use of guanidine is lim...

Elucidating the molecular basis of action of a classical drug: Guanidine compounds as inhibitors of voltage-gated potassium channels

Regulation of voltage-gated potassium channels by PI(4,5)P2

Phosphatidylinositol 4,5-bisphosphate (PI(4,5)P(2)) regulates activities of numerous ion channels including inwardly rectifying potassium (K(ir)) channels, KCNQ, TRP, and voltage-gated calcium channels. Several studies suggest that voltage-gated potassium (K(V)) channels might be regulated by PI(4,5)P(2). Wide expression of K(V) channels in different cells suggests that such regulation could ha...