Voltage-gated

Ion channels are specialized proteins embedded in the membrane. The ion selectivity of the channel is a property associated with its permeation pathway, normally called the pore. The magnitude of the current across the membrane depends on the density of channels, the conductance of the open channel, and how often the channel spends in its open position or its open probability. The salient feature of channels involved in excitable membranes is that the open probability is regulated by the transmembrane voltage or membrane potential. Changes in the membrane potential can be picked up by a voltage sensor that detects the voltage and transfers its energy to the pore to control its gate[1]. Despite their differences in ion selectivity and gating capabilities, voltage-gated channels in general share a number of structural features. They have a common structure with 24 transmembrane segments and a specialized pore region. Voltage-gated Na+ and Ca2+ channels are composed of a single pore-forming polypeptide (the alpha subunit), plus various auxiliary subunits. The alpha subunits of these channels contain four repeats of a core motif, which consists of six predicted transmembrane regions, S1-S6. Voltage-activated K+ channels are tetramers, with each subunit containing a single core motif. The ion-selective pore of these channels are formed by loops between the S5 and S6 regions, often called the P-regions or P-loops; four of these loops approach close together at the axis of the pore[2].


[1] The Voltage Sensor in Voltage-Dependent Ion Channels. F. Bezanilla. Physiol. Rev. 2000,80, 555-592.
[2] The moving parts of voltage-gated ion channels. G. Yellen. Q. Rev. Bioph. 1998, 31, 239-295.

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Axon ID Name Description From price
2979 ASP 2905 Potent, selective and orally active KCNH3 (Kv12.2) inhibitor €125.00
2243 AVE 0118 hydrochloride Potassium channel blocker (Kv1.5 (IKur), Kv4.3 (Ito), Kir3.4 (IKAch), and IKr currents) €120.00
1294 Chromanol 293B KCNQ1 channel blocker €95.00
1322 DMP 543 K+ channel blocker; Ach release stimulator €90.00
2103 Dofetilide Kv11.1 (hERG) channel blocker €85.00
1437 Flupirtine maleate Analgesic €65.00
2724 ICA-069673 KCNQ2/KCNQ3 channel opener; Anti-convulsant €90.00
3091 ICA-110381 KCNQ2/KCNQ3 channel opener; Anti-convulsant €80.00
1735 Kv1.3 Channel blocker 42 Kv1.3 potassium channel blocker €110.00
3032 LUF7244 Potent negative allosteric modulator (NAM) of the Kv11.1 (hERG) channel €140.00
2747 ML 213 KCNQ2/KCNQ4 channel opener €75.00
2615 ML252 Selective and brain penetrant KCNQ2 inhibitor €95.00
3196 ML277 Potent and selective KCNQ1 channel activator €80.00
1525 Retigabine KCNQ channel opener; Anti-convulsant €90.00
2252 Retigabine dihydrochloride KCNQ channel opener; Anti-convulsant €90.00

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