Table 1.
Parameters obtained from fitting the Hill equation to GABA, β-alanine, taurine, I4AA, and 5α-THDOC data
GABAAR subtype | EC50 (μm) | nH | Imax (nA) | n |
---|---|---|---|---|
GABA-dependent activation | ||||
α6β2(1)δ | 7 | |||
High-affinity component | 0.005 ± 0.001 | 1.16 ± 0.11 | 259.50 ± 73.96 | |
Low-affinity component | 2.29 ± 0.85 | 0.56 ± 0.05 | 479.10 ± 123.94 | |
Low expression | 2.62 ± 0.39 | 0.63 ± 0.02 | 129.06 ± 10.72 | 9 |
Intermediate expression | 0.46 ± 0.12 | 0.54 ± 0.02 | 317.39 ± 56.43 | 7 |
High expression | 0.04 ± 0.009 | 0.65 ± 0.04 | 690.60 ± 80.23 | 11 |
α6β2(0.3)δ | 1.52 ± 0.38 | 0.63 ± 0.03 | 362.80 ± 97.95 | 6 |
α6β2(0.1)δ | 1.25 ± 0.21 | 0.74 ± 0.02 | 321.67 ± 50.62 | 10 |
α1β2(1)γ2S | 2.87 ± 1.20 | 1.33 ± 0.10 | 2287.43 ± 237.76 | 7 |
α1β2(0.4)γ2S | 10.61 ± 3.27 | 1.22 ± 0.10 | 2270.33 ± 354.79 | 6 |
α1β2(0.08)γ2S | 37.20 ± 4.58 | 1.26 ± 0.14 | 974.33 ± 497.32 | 3 |
α1β2δ | 6.45 ± 0.85 | 1.14 ± 0.05 | 510.02 ± 80.43 | 9 |
α6β2γ2S | 22.30 ± 1.98 | 0.88 ± 0.14 | 484.00 ± 122.45 | 4 |
α4β2δ | 1.53 ± 0.14 | 0.85 ± 0.03 | 338.09 ± 52.61 | 11 |
α6β2δR287M | 3.71 ± 0.94 | 0.69 ± 0.18 | 44.67 ± 2.33 | 3 |
α6βY157Fδ | 13 | |||
High-affinity component | 0.37 ± 0.05 | 0.97 ± 0.04 | 355.54 ± 80.52 | |
High-affinity component | 104.65 ± 28.04 | 0.85 ± 0.14 | 389.23 ± 63.43 | |
α6βY157F (0.1)δ | 53.27 ± 13.99 | 0.94 ± 0.14 | 161.33 ± 36.99 | 3 |
I4AA-dependent activation | ||||
α6β2δ | 4 | |||
High-affinity component | 0.06 ± 0.01 | 0.82 ± 0.04 | 254.68 ± 52.02 | |
High-affinity component | 202.25 ± 17.71 | 2.61 ± 0.44 | 183.41 ± 16.77 | |
β-Alanine-dependent activation | ||||
α6β2δ | 5 | |||
High-affinity component | 1.16 ± 0.72 | 0.89 ± 0.12 | 160.61 ± 69.75 | |
High-affinity component | 594.66 ± 142.86 | 0.67 ± 0.05 | 277.94 ± 64.02 | |
Low expression | 412.14 ± 68.76 | 0.71 ± 0.03 | 302.74 ± 58.79 | 10 |
Intermediate expression | 111.86 ± 13.72 | 0.55 ± 0.15 | 426.33 ± 166.71 | 3 |
High expression | 2.56 ± 1.52 | 0.59 ± 0.16 | 945.00 ± 76.51 | 3 |
Taurine-dependent activation | ||||
α6β2δ | 3 | |||
High-affinity component | 5.80 ± 0.84 | 1.03 ± 0.05 | 225.33 ± 43.42 | |
High-affinity component | 806.67 ± 193.50 | 0.91 ± 0.29 | 205.00 ± 40.31 | |
Low expression | 1817.58 ± 865.99 | 0.69 ± 0.06 | 145.40 ± 13.31 | 4 |
Intermediate expression | 45.16 ± 25.57 | 0.55 ± 0.05 | 398.30 ± 63.92 | 3 |
High expression | 6.03 ± 1.62 | 0.90 ± 0.10 | 607.63 ± 160.86 | 4 |
5α-THDOC-dependent activation | ||||
α6β2δ | 0.89 ± 0.49 | 0.97 ± 0.06 | 550.67 ± 67.25 | 3 |