Table V.

Estimated parameters from Schemes 2, 3a, and 3b fitted to α2 GlyR single-channel data

Parameter name and unit Scheme 2 Scheme 3a Scheme 3b 
Rate constants ± CVM (%) 
α (s−1366 ± 12% 320 ± 3% 321 ± 4% 
β (s−1127,000 ± 9% 119,919 ± 7% 120,000 ± 8% 
γ1 (s−14 ± 81% 292 ± 98% – 
δ1 (s−10.134 ± 76% 0.014 ± 82% – 
γ 2 (s−14,418 ± 11% 2.1 × 10−7 ± 48% 106 ± 100% 
δ 2 (s−14,316 ± 12% 1.7 × 10−9 ± 42% 0.36 ± 100% 
γ 3 (s−1– 4,109 ± 20% 4,152 ± 19% 
δ 3 (s−1– 2,572 ± 38% 2,605 ± 38% 
kF+ (M−1s−17.9 × 106 ± 27% 3.1 × 107 ± 61% 2.4 × 107 ± 75% 
kF− (s−1677 ± 12% 719 ± 37% 659 ± 42% 
k+ (M−1s−11.04 × 105 ± 5% 0.779 × 105 ± 21% 0.781 × 105 ± 26% 
k (s−1439 ± 22% 154 ± 36% 158 ± 38% 
Equilibrium constants ± CVM (%) 
E = β/α 347 ± 6% 373 ± 4% 372 ± 4% 
F1 = δ 1/ γ 1 0.031 ± 28% 2.2 × 10−4 ± 63% – 
F2 = δ 2/ γ 2 0.977 ± 24% 0.011 ± 47% 0.017 ± 52% 
F3 = δ 3/ γ 3 – 0.573 ± 31% 0.570 ± 29% 
KR = k/k+ (µM) 4,241 ± 26% 1,879 ± 21% 1,919 ± 20% 
KF = kF−/kF+ (µM) 86 ± 37% 31 ± 21% 48 ± 29% 
KR/KF = F2/F1 46.5 ± 28%   
Predicted Popen curve parameters ± SDM 
max Popen 0.990 ± 0.006 0.993 ± 0.002 0.993 ± 0.002 
EC50 (µM) 243 ± 52 389 ± 66 400 ± 67 
nH 1.89 ± 0.005 2.49 ± 0.06 2.49 ± 0.05 
Parameter name and unit Scheme 2 Scheme 3a Scheme 3b 
Rate constants ± CVM (%) 
α (s−1366 ± 12% 320 ± 3% 321 ± 4% 
β (s−1127,000 ± 9% 119,919 ± 7% 120,000 ± 8% 
γ1 (s−14 ± 81% 292 ± 98% – 
δ1 (s−10.134 ± 76% 0.014 ± 82% – 
γ 2 (s−14,418 ± 11% 2.1 × 10−7 ± 48% 106 ± 100% 
δ 2 (s−14,316 ± 12% 1.7 × 10−9 ± 42% 0.36 ± 100% 
γ 3 (s−1– 4,109 ± 20% 4,152 ± 19% 
δ 3 (s−1– 2,572 ± 38% 2,605 ± 38% 
kF+ (M−1s−17.9 × 106 ± 27% 3.1 × 107 ± 61% 2.4 × 107 ± 75% 
kF− (s−1677 ± 12% 719 ± 37% 659 ± 42% 
k+ (M−1s−11.04 × 105 ± 5% 0.779 × 105 ± 21% 0.781 × 105 ± 26% 
k (s−1439 ± 22% 154 ± 36% 158 ± 38% 
Equilibrium constants ± CVM (%) 
E = β/α 347 ± 6% 373 ± 4% 372 ± 4% 
F1 = δ 1/ γ 1 0.031 ± 28% 2.2 × 10−4 ± 63% – 
F2 = δ 2/ γ 2 0.977 ± 24% 0.011 ± 47% 0.017 ± 52% 
F3 = δ 3/ γ 3 – 0.573 ± 31% 0.570 ± 29% 
KR = k/k+ (µM) 4,241 ± 26% 1,879 ± 21% 1,919 ± 20% 
KF = kF−/kF+ (µM) 86 ± 37% 31 ± 21% 48 ± 29% 
KR/KF = F2/F1 46.5 ± 28%   
Predicted Popen curve parameters ± SDM 
max Popen 0.990 ± 0.006 0.993 ± 0.002 0.993 ± 0.002 
EC50 (µM) 243 ± 52 389 ± 66 400 ± 67 
nH 1.89 ± 0.005 2.49 ± 0.06 2.49 ± 0.05 

Rate constants are means of fits to three data sets ± CVM. The equilibrium constants (E, F1, F2, F3, KR, and KF) are calculated for each separate fit, and means are listed here (because of the variability, the means of the equilibrium constants are not exactly the same as the ratios of the mean rate constants). Likewise, the mean values of the relative affinity of glycine for resting and flipped (KR/KF) are given. Also listed are the average max Popen, EC50, and Hill slope calculated from the fitted rate constants (±SDM). The number of free parameters: 9 out of 12 in Scheme 2, 10 out of 18 in Scheme 3a, and 9 out of 14 in Scheme 3b. Other rate constants are set by microscopic reversibility or constrained by the assumption that the binding sites are equivalent and independent.

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