Rockefeller University Press

Table 1.

Fitted parameters from concentration–response experiments

Construct	Voltage	log EC₅₀₍₁₎	EC₅₀₍₁₎	h₁	log EC₅₀₍₂₎	EC₅₀₍₂₎	h₂	I_max	Frac
	mV		µM			µM
WT	80	−6.50 (−6.52 to −6.47)	0.316	1.88 (1.69 to 2.07)	−3.38 (−3.85 to −2.91)	417	0.665 (0.341 to 0.989)	1.46 (1.29 to 1.64)	0.666 (0.566 to 0.766)
	−80	−6.09 (−6.11 to −6.06)	0.813	2.23 (1.98 to 2.47)	−3.38 (−3.85 to −2.91)	417	0.665 (0.341 to 0.989)	1.46 (1.29 to 1.64)	0.666 (0.566 to 0.766)
E702Q	80	−4.41 (−4.46 to −4.36)	38.8	1.09 (0.963 to 1.21)				1.03 (0.996 to 1.06)
	−80	−3.78 (−3.81 to −3.74)	167	1.19 (1.10 to 1.28)				1.13 (1.10 to 1.16)
K588E/E702Q	80	−5.03 (−5.08 to −4.97)	9.44	1.01 (0.910 to 1.11)				1.02 (0.987 to 1.06)
	−80	−4.44 (−4.51 to −4.38)	36	1.07 (0.963 to 1.18)				1.11 (1.05 to 1.17)
WT_WT	80	−6.68 (−6.71 to −6.65)	0.209	1.60 (1.39 to 1.81)	−3.14 (−3.97 to −2.31)	724	0.511 (0.196 to 0.826)	1.57 (1.24 to 1.89)	0.609 (0.446 to 0.772)
	−80	−6.23 (−6.26 to −6.20)	0.589	1.78 (1.57 to 1.98)	−3.14 (−3.97 to −2.31)	724	0.511 (0.196 to 0.826)	1.57 (1.24 to 1.89)	0.609 (0.446 to 0.772)
WT_E654Q	80	−6.52 (−6.59 to −6.44)	0.302	1.48 (1.18 to 1.77)	−3.76 (−4.03 to −3.49)	174	0.765 (0.304 to 1.22)	1.46 (1.35 to 1.57)	0.653 (0.546 to 0.760)
	−80	−6.11 (−6.16 to −6.05)	0.772	1.76 (1.43 to 2.08)	−3.76 (−4.03 to −3.49)	174	0.765 (0.304 to 1.22)	1.46 (1.35 to 1.57)	0.653 (0.546 to 0.760)
WT_E702Q (biphasic; no constraints)	80	−6.28 (−6.33 to −6.22)	0.525	1.78 (1.45 to 2.12)	−4.12 (−4.18 to −4.06)	75.9	0.851 (0.754 to 0.948)	1.00 (0.978 to 1.02)	0.312 (0.284 to 0.340)
	−80	−5.89 (−5.95 to −5.83)	1.29	1.96 (1.61 to 2.31)	−3.72 (−3.76 to −3.68)	191	1.21 (1.06 to 1.37)	1.00 (0.978 to 1.02)	0.312 (0.284 to 0.340)
WT_E702Q (triphasic; A = 0.6, log EC₅₀₍₃₎ = −3.14, h₃ = 0.511, h₁ = 1.88, h₂ = 1.09)	80	−6.26 (−6.31 to −6.21)	0.548	=1.88	−4.21 (−4.29 to −4.13)	61.8	=1.09	1.25 (1.22 to 1.27)	0.517 (0.495 to 0.538)
	−80	−5.92 (−5.97 to −5.87)	1.20	=2.23	−3.77 (−3.82 to −3.72)	171	=1.19	1.41 (1.38 to 1.44)	0.444 (0.424 to 0.463)
WT_E702Q (triphasic; A = 0.6, log EC₅₀₍₃₎ = −3.14, h₃ = 0.511)	80	−6.29 (−6.34 to −6.23)	0.514	1.88 (1.52 to 2.24)	−4.24 (−4.30 to −4.17)	58	0.921 (0.795 to 1.05)	1.06 (1.04 to 1.07)	0.477 (0.442 to 0.513)
	−80	−5.88 (−5.94 to −5.82)	1.32	1.99 (1.63 to 2.36)	−3.75 (−3.79 to −3.70)	179	1.36 (1.15 to 1.57)	1.06 (1.04 to 1.07)	0.477 (0.442 to 0.513)
K588E_E702Q (biphasic; log EC₅₀₍₁₎ = −6.46, h₁ = 1.42)	80	= −6.46	=0.347	=1.42	−4.28 (−4.34 to −4.21)	52.5	1.13 (1.01 to 1.24)	1.16 (1.10 to 1.22)	0.015 (0.0055 to 0.024)
	−80				−3.79 (−3.80 to −3.77)	163.2	1.49 (1.44 to 1.55)	1.40 (1.39 to 1.42)
WT_K588E/E702Q (biphasic)	80	−6.29 (−6.41 to −6.17)	0.513	1.56 (0.811 to 2.30)	−4.20 (−4.61 to −3.79)	63.1	0.616 (0.229 to 1.00)	1.20 (1.08 to 1.31)	0.412 (0.176 to 0.648)
	−80	−5.97 (−6.05 to −5.88)	1.07	1.82 (1.39 to 2.24)	−3.82 (−4.03 to −3.61)	151	1.11 (0.505 to 1.71)	1.15 (1.08 to 1.22)	0.599 (0.506 to 0.692)

Construct	Voltage	log EC₅₀₍₁₎	EC₅₀₍₁₎	h₁	log EC₅₀₍₂₎	EC₅₀₍₂₎	h₂	I_max	Frac
	mV		µM			µM
WT	80	−6.50 (−6.52 to −6.47)	0.316	1.88 (1.69 to 2.07)	−3.38 (−3.85 to −2.91)	417	0.665 (0.341 to 0.989)	1.46 (1.29 to 1.64)	0.666 (0.566 to 0.766)
	−80	−6.09 (−6.11 to −6.06)	0.813	2.23 (1.98 to 2.47)	−3.38 (−3.85 to −2.91)	417	0.665 (0.341 to 0.989)	1.46 (1.29 to 1.64)	0.666 (0.566 to 0.766)
E702Q	80	−4.41 (−4.46 to −4.36)	38.8	1.09 (0.963 to 1.21)				1.03 (0.996 to 1.06)
	−80	−3.78 (−3.81 to −3.74)	167	1.19 (1.10 to 1.28)				1.13 (1.10 to 1.16)
K588E/E702Q	80	−5.03 (−5.08 to −4.97)	9.44	1.01 (0.910 to 1.11)				1.02 (0.987 to 1.06)
	−80	−4.44 (−4.51 to −4.38)	36	1.07 (0.963 to 1.18)				1.11 (1.05 to 1.17)
WT_WT	80	−6.68 (−6.71 to −6.65)	0.209	1.60 (1.39 to 1.81)	−3.14 (−3.97 to −2.31)	724	0.511 (0.196 to 0.826)	1.57 (1.24 to 1.89)	0.609 (0.446 to 0.772)
	−80	−6.23 (−6.26 to −6.20)	0.589	1.78 (1.57 to 1.98)	−3.14 (−3.97 to −2.31)	724	0.511 (0.196 to 0.826)	1.57 (1.24 to 1.89)	0.609 (0.446 to 0.772)
WT_E654Q	80	−6.52 (−6.59 to −6.44)	0.302	1.48 (1.18 to 1.77)	−3.76 (−4.03 to −3.49)	174	0.765 (0.304 to 1.22)	1.46 (1.35 to 1.57)	0.653 (0.546 to 0.760)
	−80	−6.11 (−6.16 to −6.05)	0.772	1.76 (1.43 to 2.08)	−3.76 (−4.03 to −3.49)	174	0.765 (0.304 to 1.22)	1.46 (1.35 to 1.57)	0.653 (0.546 to 0.760)
WT_E702Q (biphasic; no constraints)	80	−6.28 (−6.33 to −6.22)	0.525	1.78 (1.45 to 2.12)	−4.12 (−4.18 to −4.06)	75.9	0.851 (0.754 to 0.948)	1.00 (0.978 to 1.02)	0.312 (0.284 to 0.340)
	−80	−5.89 (−5.95 to −5.83)	1.29	1.96 (1.61 to 2.31)	−3.72 (−3.76 to −3.68)	191	1.21 (1.06 to 1.37)	1.00 (0.978 to 1.02)	0.312 (0.284 to 0.340)
WT_E702Q (triphasic; A = 0.6, log EC₅₀₍₃₎ = −3.14, h₃ = 0.511, h₁ = 1.88, h₂ = 1.09)	80	−6.26 (−6.31 to −6.21)	0.548	=1.88	−4.21 (−4.29 to −4.13)	61.8	=1.09	1.25 (1.22 to 1.27)	0.517 (0.495 to 0.538)
	−80	−5.92 (−5.97 to −5.87)	1.20	=2.23	−3.77 (−3.82 to −3.72)	171	=1.19	1.41 (1.38 to 1.44)	0.444 (0.424 to 0.463)
WT_E702Q (triphasic; A = 0.6, log EC₅₀₍₃₎ = −3.14, h₃ = 0.511)	80	−6.29 (−6.34 to −6.23)	0.514	1.88 (1.52 to 2.24)	−4.24 (−4.30 to −4.17)	58	0.921 (0.795 to 1.05)	1.06 (1.04 to 1.07)	0.477 (0.442 to 0.513)
	−80	−5.88 (−5.94 to −5.82)	1.32	1.99 (1.63 to 2.36)	−3.75 (−3.79 to −3.70)	179	1.36 (1.15 to 1.57)	1.06 (1.04 to 1.07)	0.477 (0.442 to 0.513)
K588E_E702Q (biphasic; log EC₅₀₍₁₎ = −6.46, h₁ = 1.42)	80	= −6.46	=0.347	=1.42	−4.28 (−4.34 to −4.21)	52.5	1.13 (1.01 to 1.24)	1.16 (1.10 to 1.22)	0.015 (0.0055 to 0.024)
	−80				−3.79 (−3.80 to −3.77)	163.2	1.49 (1.44 to 1.55)	1.40 (1.39 to 1.42)
WT_K588E/E702Q (biphasic)	80	−6.29 (−6.41 to −6.17)	0.513	1.56 (0.811 to 2.30)	−4.20 (−4.61 to −3.79)	63.1	0.616 (0.229 to 1.00)	1.20 (1.08 to 1.31)	0.412 (0.176 to 0.648)
	−80	−5.97 (−6.05 to −5.88)	1.07	1.82 (1.39 to 2.24)	−3.82 (−4.03 to −3.61)	151	1.11 (0.505 to 1.71)	1.15 (1.08 to 1.22)	0.599 (0.506 to 0.692)

Asymptotic 95% confidence intervals are in parentheses; values preceded by = were constrained during fitting; values that are identical at 80 and −80 mV were constrained to a shared but freely varying value; data at 80 and −80 mV were normalized to their respective I_max values before global fitting.

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