Table 1.

Desensitization parameters for WT and mutant GluAZ flip and flop receptors with four modulators.

GluA2i	Wild-type	S₄₉₇A	S₄₉₇T	S₇₂₉A	G₇₃₁A	K₇₆₃Q
*10 mM Glu*
Weighted τ_des	6.7 ± 0.4 (22)	11.1 ± 2.2*** (5)	6.7 ± 0.2 (4)	6.2 ± 1.2 (4)	0.54 ± 0.03*** (15)	4.6 ± 0.3* (18)
% fast-component τ_des	51.8 ± 5.4	70.1 ± 9.5	68.9 ±10.2	57.4 ± 20.5	88.8 ± 2.7***	56.7 ± 5.8
% Des	96.3 ± 0.8	90.4 ± 4.8*	97.9 ± 0.4	98.9 ± 0.5	96.8 ± 0.8	96.8 ± 0.6
Weighted τ_deact	0.8 ± 0.1 (21)	1.2 ± 0.4 (4)	1.0 ± 0.1 (4)	1.1 ± 0.3 (3)	0.4 ± 0.04* (15)	1.0 ± 0.1 (15)
% fast-component τ_deact	55.4 ± 6.3	79.2 ± 5.4	49.3 ± 17.3	54.6 ± 28.7	64.9 ± 6.5	78.9 ± 5.8
10 μM CMPDA
Weighted τ_des	Non-Des (5)	Non-Des (1)	Non-Des (5)	Non-Des (2)	8.8 ± 2.3 (7)	Non-Des (8)
% fast-component τ_des	Non-Des	Non-Des	Non-Des	Non-Des	92.6 ± 0.7*	Non-Des
% Des	8.0 ± 2.9^†††	9.6 ± 0^†††	1.2 ± 0.6^†††	−1.0 ± 0.4^†††	95.5 ± 0.6***	8.4 ± 2.8^†††
Weighted τ_deact	1.8 ± 0.3 (5)	7.8 ± 0^†††* (1)	3.2 ± 1.2 (5)	6.1 ± 0.7^†* (2)	0.4 ± 0.07 (7)	4.1 ± 0.7^††† (7)
% fast-component τ_deact	53.1 ± 10.4	73.3 ± 0	35.3 ± 11.8	28.4 ± 8.8	81.8 ± 5.7	35.1 ± 7.8^††
**100 μM CX614**
Weighted τ_des	46.5 ± 12.0^† (10)	Non-Des (4)	65.0 ± 18.0^† (3)	114 ± 9.0^†††* (4)	0.9 ± 0.1 (6)	62.9 ± 16.5^† (9)
% fast-component τ_des	76.6 ± 3.4^†	Non-Des	66.9 ± 7.6	65.2 ± 3.7	76.3 ± 9.0	64.6 ± 4.4
% Des	34.4 ± 5.5^†††	10.7 ± 1.3^†††*	21.3 ± 6.0^†††	71.0 ± 2.7^†††***	94.9 ± 2.3***	61.1 ± 2.8^†††***
Weighted τ_deact	1.9 ± 0.7 (10)	4.2 ± 0.7^†* (4)	1.3 ± 0.02 (3)	1.3 ± 0.1 (4)	0.5 ± 0.06 (6)	2.2 ± 0.3^† (9)
% fast-component τ_deact	77.0 ± 6.8	41.9 ± 6.7^†*	74.4 ± 5.7	62.3 ± 4.6	49.5 ± 11.4*	65.1 ± 5.9
10 μM CMPDB
Weighted τ_des	49.0 ± 20.8^† (7)	29.1 ± 2.8 (3)	Non-Des (6)	Non-Des (5)	6.3 ± 1.6* (8)	5.3 ± 0.2* (7)
% fast-component τ_des	57.6 ± 4.8	83.2 ± 1.3*	Non-Des	Non-Des	89.6 ± 2.2***	73.6 ± 6.4
% Des	34.4 ± 10.9^†††	33.7 ± 1.0^†††	21.1 ± 1.4^†††	13.3 ± 0.8^†††*	93.7 ± 0.9***	94.4 ± 0.9***
Weighted τ_deact	5.6 ± 1.2^††† (7)	3.7 ± 0.4^† (3)	3.6 ± 0.7 (6)	5.3 ± 1.4^† (5)	0.5 ± 0.04*** (8)	1.4 ± 0.3* (7)
% fast-component τ_deact	43.9 ± 10.2	29.3 ± 9.9^†	50.5 ± 10.9	38.4 ± 8.3	61.6 ± 6.5	68.3 ± 10.2
**100 μM CTZ**
Weighted τ_des	Non-Des (8)	Non-Des (9)	Non-Des (3)	Non-Des (6)	86.6 ± 35.6^††† (6)	Non-Des (13)
% fast-component τ_des	Non-Des	Non-Des	Non-Des	Non-Des	39.7 ± 14.3^†††	Non-Des
% Des	4.3 ± 2.3^†††	8.3 ± 1.9^†††	0.9 ± 0.6^†††	8.9 ± 1.8^†††	27.7 ± 6.5^†††***	20.3 ± 2.8^†††*
Weighted τ_deact	1.3 ± 0.3 (8)	1.4 ± 0.3 (6)	1.9 ± 0.2 (3)	2.6 ± 0.5* (6)	0.8 ± 0.09^†† (6)	2.2 ± 0.2* (12)
% fast-component τ_deact	49.5 ± 12.1	75.5 ± 8.5	43.4 ± 4.2	36.5 ± 11.2	54.6 ± 6.7	51.6 ± 7.2^†

GluA2o	Wild-type	S₄₉₇A	S₄₉₇T	S₇₂₉A	G₇₃₁A	K₇₆₃Q
*10 mM Glu*
Weighted τ_des	1.6 ± 0.1 (22)	2.0 ± 0.1 (7)	3.0 ± 0.7*** (3)	1.0 ± 0.1* (5)	0.8 ± 0.1*** (9)	1.0 ± 0.1*** (25)
% fast-component τ_des	56.6 ± 4.5	58.9 ± 8.9	12.8 ± 5.8*	37.4 ± 10.6	76.5 ± 4.5	71.7 ± 4.0
% Des	97.1 ± 0.7	95.8 ± 1.3	97.5 ± 1.9	99.2 ± 0.2	96.7 ± 1.1	98.0 ± 0.3
Weighted τ_deact	0.7 ± 0.07 (18)	1.0 ± 0.1 (7)	1.0 ± 0.3 (3)	0.6 ± 0.05 (5)	0.5 ± 0.1 (9)	0.7 ± 0.05 (23)
% fast-component τ_deact	62.0 ± 6.2	24.0 ± 5.4*	24.2 ± 10.1*	28.9 ± 3.2*	75.6 ± 5.5	49.7 ± 5.4
10 μM CMPDA
Weighted τ_des	Non-Des (12)	Non-Des (6)	15.6 ± 5.7 (3)	Non-Des (4)	1.1 ±0.2 (7)	Non-Des (6)
% fast-component τ_des	Non-Des	Non-Des	90.0 ± 3.7^††	Non-Des	79.2 ± 2.5	Non-Des
% Des	6.1 ± 1.1^†††	11.2 ± 1.7^†††	40.4 ± 2.8^†††***	8.9 ± 4.0^†††	97.5 ± 0.7***	4.8 ± 1.1^†††
Weighted τ_deact	2.8 ± 0.4^† (12)	3.6 ± 0.5^††† (6)	3.5 ± 0.4^†† (3)	3.4 ± 0.8 (6)	0.3 ± 0.02* (7)	7.0 ± 1.2^†††*** (6)
% fast-component τ_deact	45.6 ± 5.0	24.6 ± 6.7*	22.5 ± 4.7	27.9 ± 7.2	71.2 ± 4.5*	32.4 ± 6.8
**100 μM CX614**
Weighted τ_des	121 ± 24.3^††† (12)	Non-Des (3)	2.1 ± 0.5* (3)	108.5 ± 37.9 (5)	1.0 ± 0.1* (7)	120.9 ± 14.4^††† (8)
% fast-component τ_des	31.1 ± 5.2^††	Non-Des	55.0 ± 1.0^†	34.5 ± 16.7	74.7 ± 3.2***	26.1 ± 4.3^†††
% Des	33.4 ± 2.1^†††	10.5 ± 2.1^†††***	94.8 ± 1.4***	86.3 ± 1.8^†***	93.9 ± 1.8***	76.8 ± 2.4^†††***
Weighted τ_deact	2.4 ± 0.5^† (14)	6.1 ± 0.9^†††* (3)	0.8 ± 0.06 (3)	2.7 ± 1.0 (5)	0.5 ± 0.06* (8)	4.3 ± 0.5^†††* (8)
% fast-component τ_deact	37.6 ± 4.5^†	4.0 ± 2.0*	97.5 ± 1.0^††***	44.9 ± 15.8	59.0 ± 5.2*	43.9 ± 1.2
10 μM CMPDB
Weighted τ_des	2.3 ± 0.2 (11)	2.4 ± 0.4 (3)	1.9 ± 0.2 (3)	134.1 ± 45.4*** (3)	1.5 ± 0.3 (8)	0.9 ± 0.1 (9)
% fast-component τ_des	92.1 ± 2.6^†††	90.0 ± 2.5	58.9 ± 19.9^†*	32.9 ± 8.2***	71.3 ± 6.6	69.7 ± 6.8*
% Des	81.5 ± 3.6^†††	75.1 ± 7.3^††	99.2 ± 0.5*	43.5 ± 3.2^†††***	92.8 ± 2.8*	97.4 ± 0.6*
Weighted τ_deact	3.7 ± 1.5^†† (7)	1.4 ± 0.2 (2)	0.9 ± 0.06 (3)	7.3 ± 1.8^†† (3)	0.3 ± 0.03* (8)	0.6 ± 0.02* (8)
% fast-component τ_deact	72.0 ± 13.9	79.8 ± 6.1^††	59.1 ± 10.5	13.6 ± 3.9*	76.6 ± 6.1	38.0 ± 4.3*
**100 μM CTZ**
Weighted τ_des	153 ± 12.3^††† (8)	148.6 ± 13.5^††† (6)	91.2 ± 14.0^†††* (4)	85.2 ± 9.1* (2)	54.6 ± 4.7^†††*** (8)	52.4 ± 4.9^†††*** (8)
% fast-component τ_des	11.9 ± 2.5^†††	13.9 ± 8.0^†	15.5 ± 7.9	21.6 ± 4.1	26.2 ± 2.2^†††	35.5 ± 2.9^†††***
% Des	67.3 ± 5.1^†††	85.0 ± 2.8^†*	95.1 ± 1.6*	93.3 ± 1.8*	93.3 ± 2.9**	87.6 ± 6.0^†*
Weighted τ_deact	0.6 ± 0.07 (8)	0.6 ± 0.1 (6)	0.9 ± 0.4 (4)	0.7 ± 0.06 (2)	1.2 ± 0.3^† (8)	0.8 ± 0.07 (8)
% fast-component τ_deact	59.1 ± 9.6	42.3 ± 7.1	37.0 ± 11.2	77.1 ± 9.9^†	41.6 ± 11.71^†	55.3 ± 6.4

WT, but not mutant, data are reused from Timm et al. (2011) with permission from Molecular Pharmacology.