Table 4.
Ions and molecules tested as gating pore blockers.
| Channel | Mutation | Location | Ions | Guanidinium derivatives | References | ||
|---|---|---|---|---|---|---|---|
| Block | No effect | Block | No effect | ||||
| dShaker | R362C/E283D | R1/E1 | Mg2+ | Ethyl-guanidium | Tombola et al., 2005 | ||
| rNav1.4 | R666G | DII/R2 | Ca2+, Zn2+, Ba2+ | Sokolov et al., 2007 | |||
| rNav1.4 | R663H | DII/R1 | Li+, Ni2+, Cd2+, Ba2+ | Struyk and Cannon, 2007 | |||
| rNav1.4 | R666G | DII/R2 | Ca2+, Zn2+, Ba2+ | Struyk et al., 2008 | |||
| N.at-Kv3.2 | None* | None* | Ba2+ | Klassen et al., 2008 | |||
| rNav1.4 | R666G | DII/R2 | Ca2+, Zn2+, Y3+, Ba2+, La3+, Yb3+, Lu3+, Hf4+, Tl3+ | 1-(2,4-xylyl) guanidine-carbonate | Ethyl- guanidium | Sokolov et al., 2010 | |
| hHv1 | R211S | R3 | Zn2+ | Berger and Isacoff, 2011 | |||
| rNav1.4 | R1125Q | DIII/R2 | Ni2+, Zn2+ | Ca2+, Ba2+ | Francis et al., 2011 | ||
| hNav1.5 | R219H | DI/R1 | Ni2+, Zn2+, Cd2+,La3+ | Ethyl- guanidium | Gosselin-Badaroudine et al., 2012b | ||
For N.at-Kv3.2, no substitution was required to induce a gating pore.