TABLE 3

Summary of hypotheses related to inhibitory mechanisms

AgentVoltage DependenceComments
ControlPNU-120596
MecamylamineNet charge onlyStrongIn 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-314StrongNoneFast channel blocker, no subconductance events. However, since burst durations are decreased, there must be some long block times as well.
TetracaineNoneNoneMost 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.
BTMPSNet charge onlyPeak onlyInhibition 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.
TMPHPeak onlyStrongLikely to preferentially block open channels; however, the off-rate for α7 receptors is relatively fast compared with what has been reported for heteromeric channels.
tkP3BzPBNoneWeakProbably not an open channel blocker. Shows preferential inhibition of the PNU-120596–potentiated receptors. Probably affects channels in both closed and open states.