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. 2013 Sep;84(3):459–475. doi: 10.1124/mol.113.086462

TABLE 3.

Summary of hypotheses related to inhibitory mechanisms

Agent Voltage Dependence
Comments
Control PNU-120596
Mecamylamine Net charge only Strong In the presence of the PAM, decreases open times and burst durations. Produces small-amplitude subconductance events. Most likely open channel block but produces some longer block times as well.
QX-314 Strong None Fast channel blocker, no subconductance events. However, since burst durations are decreased, there must be some long block times as well.
Tetracaine None None Most likely blocks both open and closed channels. Multiple forms of blockade suggested by closed times, the increase in burst frequency, and the appearance of subconductance states.
BTMPS Net charge only Peak only Inhibition is use-dependent but not strongly voltage dependent. The longer channels are open, as in the presence of the PAM, the more likely they are to be blocked.
TMPH Peak only Strong Likely to preferentially block open channels; however, the off-rate for α7 receptors is relatively fast compared with what has been reported for heteromeric channels.
tkP3BzPB None Weak Probably not an open channel blocker. Shows preferential inhibition of the PNU-120596–potentiated receptors. Probably affects channels in both closed and open states.