Table 1. Biophysical characteristics of... | Rockefeller University Press

Table 1.

Biophysical characteristics of WT and R56Q mutant channels in the absence and presence of RPR260243 (RPR) at 21°C and 37°C

		RPR	Activation		Deactivation (at −110 mV for 21°C, at −60 mV for 37°C)			Inactivation		Inactivation recovery
		RPR	V_1/2 (mV)	k (mV)	τ_fast (ms)	τ_slow (ms)	% A_fast	V_1/2 (mV)	k (mV)	τ_-90mV (ms)
21°C	WT	Ctrl	−11.9 ± 2.8	10.3 ± 0.8	36.4 ± 10.6	166.8 ± 134	81 ± 5.9	−55.8 ± 6.1	−19.2 ± 0.9	8.8 ± 3.7
		1 µM	-	-	36.2 ± 5.9	182.8 ± 54	83 ± 4.4	-	-	-
		3 µM	-	-	28.5 ± 7.8	221.7 ± 102	86 ± 2.7	-	-	-
		10 µM	−14.1 ± 3.4^a	10.6 ± 0.7	40.9 ± 3.1	953.7 ± 252^a	79 ± 4.6	−44.0 ± 6.6^a	−17.6 ± 0.8	4.2 ± 1.3
	R56Q	Ctrl	−10.5 ± 2.7	10.5 ± 0.3	15.7 ± 1.6^b	114.0 ± 20.9^b	94 ± 2.7^b	−41.5 ± 8.5^b	−19.6 ± 2.3	5.5 ± 2.3
		1 µM	-	-	14.9 ± 0.4	166.6 ± 30.1	95 ± 0.8	-	-	-
		3 µM	-	-	17.2 ± 1.8	188.0 ± 31.4	89 ± 1.5	-	-	-
		10 µM	−12.3 ± 3.2^a	10.7 ± 0.6	20.1 ± 0.9	223.2 ± 16.1	85 ± 1.9^a	−40.5 ± 8.3	−20.4 ± 1.6	6.3 ± 2.7
37°C	WT	Ctrl	−25.8 ± 3.1	6.2 ± 0.6	161 ± 43	866.8 ± 288	55 ± 7.3	−34.3 ± 10.4	−20.0 ± 0.5	1.5 ± 0.3
		1 µM	-	-	162 ± 24	1,595 ± 124	40 ± 6.3^a	-	-	-
		3 µM	-	-	129 ± 35	2,526 ± 231	20 ± 4.8^a	-	-	-
		10 µM	−26.5 ± 3.4	5.9 ± 0.7	54.9 ± 14^a	6,029 ± 2,699^a	7.2 ± 3.9^a	−27.1 ± 6.8	−19.3 ± 1.7	1.6 ± 0.3
	R56Q	Ctrl	−15.8 ± 3.9^b	7.9 ± 2.3	43.5 ± 5.1^b	539.8 ± 322	93 ± 5.7^b	−10.9 ± 16.9^b	−19.9 ± 2.1	1.4 ± 1.1
		1 µM	-	-	50.2 ± 8.2	1,440 ± 276	74 ± 4.3^a	-	-	-
		3 µM	-	-	59.8 ± 8.5	1,850 ± 432	51 ± 5.7^a	-	-	-
		10 µM	−21.5 ± 6.0^a	7.1 ± 1.6	46.0 ± 10	1,520 ± 533	37 ± 10.5^a	−15.0 ± 14.7	−17.8 ± 4.4	1.7 ± 1.4

		RPR	Activation		Deactivation (at −110 mV for 21°C, at −60 mV for 37°C)			Inactivation		Inactivation recovery
		RPR	V_1/2 (mV)	k (mV)	τ_fast (ms)	τ_slow (ms)	% A_fast	V_1/2 (mV)	k (mV)	τ_-90mV (ms)
21°C	WT	Ctrl	−11.9 ± 2.8	10.3 ± 0.8	36.4 ± 10.6	166.8 ± 134	81 ± 5.9	−55.8 ± 6.1	−19.2 ± 0.9	8.8 ± 3.7
		1 µM	-	-	36.2 ± 5.9	182.8 ± 54	83 ± 4.4	-	-	-
		3 µM	-	-	28.5 ± 7.8	221.7 ± 102	86 ± 2.7	-	-	-
		10 µM	−14.1 ± 3.4^a	10.6 ± 0.7	40.9 ± 3.1	953.7 ± 252^a	79 ± 4.6	−44.0 ± 6.6^a	−17.6 ± 0.8	4.2 ± 1.3
	R56Q	Ctrl	−10.5 ± 2.7	10.5 ± 0.3	15.7 ± 1.6^b	114.0 ± 20.9^b	94 ± 2.7^b	−41.5 ± 8.5^b	−19.6 ± 2.3	5.5 ± 2.3
		1 µM	-	-	14.9 ± 0.4	166.6 ± 30.1	95 ± 0.8	-	-	-
		3 µM	-	-	17.2 ± 1.8	188.0 ± 31.4	89 ± 1.5	-	-	-
		10 µM	−12.3 ± 3.2^a	10.7 ± 0.6	20.1 ± 0.9	223.2 ± 16.1	85 ± 1.9^a	−40.5 ± 8.3	−20.4 ± 1.6	6.3 ± 2.7
37°C	WT	Ctrl	−25.8 ± 3.1	6.2 ± 0.6	161 ± 43	866.8 ± 288	55 ± 7.3	−34.3 ± 10.4	−20.0 ± 0.5	1.5 ± 0.3
		1 µM	-	-	162 ± 24	1,595 ± 124	40 ± 6.3^a	-	-	-
		3 µM	-	-	129 ± 35	2,526 ± 231	20 ± 4.8^a	-	-	-
		10 µM	−26.5 ± 3.4	5.9 ± 0.7	54.9 ± 14^a	6,029 ± 2,699^a	7.2 ± 3.9^a	−27.1 ± 6.8	−19.3 ± 1.7	1.6 ± 0.3
	R56Q	Ctrl	−15.8 ± 3.9^b	7.9 ± 2.3	43.5 ± 5.1^b	539.8 ± 322	93 ± 5.7^b	−10.9 ± 16.9^b	−19.9 ± 2.1	1.4 ± 1.1
		1 µM	-	-	50.2 ± 8.2	1,440 ± 276	74 ± 4.3^a	-	-	-
		3 µM	-	-	59.8 ± 8.5	1,850 ± 432	51 ± 5.7^a	-	-	-
		10 µM	−21.5 ± 6.0^a	7.1 ± 1.6	46.0 ± 10	1,520 ± 533	37 ± 10.5^a	−15.0 ± 14.7	−17.8 ± 4.4	1.7 ± 1.4

Ctrl, control.

Significant difference compared to control (drug versus control).

Significant difference compared to construct (R56Q versus WT).