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. |