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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1816 A 784168 TRPV1 receptor antagonist €95.00
1504 ABT 102 TRPV1 antagonist €90.00
3356 AMG 9810 Potent and selective vanilloid receptor-1 (TRPV1) antagonist €90.00
2742 GSK 2193874 Orally active TRPV4 antagonist €120.00
2423 M8-B hydrochloride Selective and potent antagonist of the TRPM8 channel €115.00
2980 ML2-SA1 Potent and selective activator of TRPML2 €105.00
2374 Optovin Reversible photoactivated TRPA1 agonist €85.00
2483 PF 05105679 TRPM8 inhibitor with >100-fold selectivity and in vivo activity in humans €90.00
2498 RQ 00203078 Selective, potent, and orally active TRPM8 antagonist with in vivo activity €125.00

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