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
3254 Nicardipine Ca2+ channel antagonist €50.00
2068 Nifedipine Ca2+ channel blocker (L-type voltage gated) €55.00
3349 NMDAR-TRPM4 blocker C19 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €130.00
3348 NMDAR-TRPM4 blocker C8 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €120.00
2374 Optovin Reversible photoactivated TRPA1 agonist €85.00
3158 Otilonium bromide Ca2+ channel blocker €70.00
2483 PF 05105679 TRPM8 inhibitor with >100-fold selectivity and in vivo activity in humans €90.00
1823 Pregabalin Reduces synaptic signaling by binding to α2δ subunits €85.00
3507 Ranolazine Ca2+/K+/Na+ channel blocker; Anti-anginal agent  Recently added €70.00
1525 Retigabine KCNQ channel opener; Anti-convulsant €90.00
2252 Retigabine dihydrochloride KCNQ channel opener; Anti-convulsant €90.00
2498 RQ 00203078 Selective, potent, and orally active TRPM8 antagonist with in vivo activity €125.00
1657 S 9947 Ikur/Kv1.5 channel Inhibitor €125.00
1221 SKF 96365 hydrochloride Ca2+ channel blocker €105.00
3452 Verapamil hydrochloride Ca2+ channel antagonist  Recently added €50.00

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