Table 1.

Inhibition Constants of BDZ-f Obtained from Rate and Amplitude Measurements for the Closed- and Open-Channel States of GluA2Q_flip

	Rate Measurementa		Amplitude Measurement
Inhibitor	$K_I^{*}$ (µM)b (closed channel)	${\overline{K}}_I^{*}$ (µM)b (open channel)	KI (µM)b,d	KI (µM)b,e	KI (µM)c,d (closed channel)	K̅I (µM)c,f (open channel)
BDZ-f	22 ± 1	20 ± 3	4.0 ± 0.2	4.7 ± 0.3	3.8 ± 0.4	5.4 ± 0.8
GYKI 52466g	61 ± 11	128 ± 30	15 ± 1	16 ± 1	14 ± 1	30 ± 2
BDZ-3h	514 ± 60	204 ± 18	200 ± 18	69 ± 4	210 ± 20	38 ± 10

^aThe constants obtained from rate measurements represent those in the first step of inhibition as in Figure 4, whereas those obtained from the amplitude measurements represent the overall inhibition constants.

^bLaser-pulse photolysis measurement.

^cFlow measurement.

^dMeasurements at 100 µM glutamate for the closed-channel state.

^eMeasurements at ~300 µM glutamate.

^fMeasurements at 3 mM glutamate.

^gRitz et al (2011), in press.

^hRitz et al, 2008.