Table 2.

Efficacy and Occupancy Analysis

Receptor + Drug	Decay to 95% (ms)	I_C/I_B (%) (efficacy)	1 – (I_A – I_B)/I_A (%) (occupancy)	n
GluA2i WT	29			22
+ CTZ		101.4 ± 2.0	91.9 ± 2.1	8
+ CX614		114.7 ± 4.4	55.1 ± 4.3	10
+ CMPDA		95.7 ± 2.4	93.6 ± 1.8	5
+ CMPDB		94.8 ± 1.7	83.8 ± 1.4	7
GluA2i S₄₉₇A	31			5
+ CTZ		98.9 ± 2.1	87.9 ± 1.9	9
+ CX614		103.1 ± 2.8	85.0 ± 1.5	4
+ CMPDA		91.1	92.3	1
+ CMPDB		102.9 ± 4.5	65.1 ± 2.0	3
GluA2i S₄₉₇T	26			4
+ CTZ		103.9 ± 1.9	91.3 ± 4.2	3
+ CX614		130.2 ± 1.5	59.0 ± 4.8	3
+ CMPDA		100.0 ± 0.8	96.9 ± 0.8	5
+ CMPDB		97.3 ± 1.6	77.5 ± 2.4	6
GluA2i S₇₂₉A	19			4
+ CTZ		96.3 ± 3.4	94.2 ± 3.5	6
+ CX614		57.6 ± 4.9	50.7 ± 1.5	4
+ CMPDA		101.3	98.7	2
+ CMPDB		95.0 ± 2.0	90.8 ± 1.7	5
GluA2i G₇₃₁A	2			15
+ CTZ		88.2 ± 2.5	90.5 ± 3.5	5
+ CX614		25.8 ± 5.6	16.8 ± 3.3	5
+ CM PDA		24.3 ± 10.6	13.1 ± 2.8	5
+ CMPDB		29.8 ± 3.5	16.7 ± 1.6	8
GluA2i K₇₆₃Q	15			18
+ CTZ		94.6 ± 1.4	81.0 ± 1.6	13
+ CX614		66.3 ± 4.5	56.8 ± 1.2	9
+ CMPDA		93.6 ± 2.4	95.4 ± 1.2	8
+ CMPDB		63.2 ± 16.7	13.6 ± 2.0	7
GluA2o WT	5			22
+ CTZ		31.0 ± 5.4	88.1 ± 2.8	7
+ CX614		72.9 ± 2.6	88.9 ± 1.5	12
+ CMPDA		103.6 ± 4.7	90.6 ± 2.3	12
+ CMPDB		68.3 ± 2.6	26.1 ± 4.2	11
GluA2o S₄₉₇A	7			7
+ CTZ		18.4 ± 1.9	95.3 ± 1.9	6
+ CX614		92.6 ±2.2	94.9 ± 1.4	3
+ CMPDA		98.8 ± 0.8	87.2 ± 3.6	4
+ CMPDB		93.1 ± 11.6	30.6 ± 4.3	3
GluA2o S₄₉₇T	10			3
+ CTZ		6.3 ± 1.4	75.0 ± 5.5	4
+ CX614		66.9 ± 7.2	4.4 ± 0.5	3
+ CMPDA		99.2 ± 3.2	67.2 ± 3.8	3
+ CMPDB		24.0 ± 3.6	5.2 ± 3.5	3
GluA2o S₇₂₉A	3			5
+ CTZ		5.9	92.7	2
+ CX614		14.9 ± 1.3	80.8 ± 8.5	4
+ CMPDA		87.6 ± 2.4	96.6 ± 0.9	5
+ CMPDB		65.5 ± 2.6	82.8 ± 2.4	3
GluA2o G₇₃₁A	3			9
+ CTZ		3.5 ± 1.4	83.9 ± 2.6	7
+ CX614		27.7 ± 3.6	11.4 ± 1.4	5
+ CMPDA		20.6 ± 5.1	16.8 ± 1.3	6
+ CMPDB		24.8 ± 3.2	15.0 ± 2.0	6
GluA2o K₇₆₃Q	3			25
+ CTZ		5.2 ± 1.4	78.0 ± 3.6	8
+ CX614		29.2 ± 2.7	75.1 ± 1.3	8
+ CMPDA		97.3 ± 1.7	93.6 ±2.0	6
+ CMPDB		42.8 ± 8.6	7.7 ± 0.9	9