Table 3.
GABAA receptor subtype | Single-channel conductance (pS) | GABA EC50 (µM) | Hill coefficient | Characteristic time of desensitization td (s) | Characteristic time of deactivation (ms) | Activation time (ms) |
---|---|---|---|---|---|---|
α1β1γ1 | 5.2 [165] | |||||
α1β1γ2 |
30 [125] (γ2L splice variant) 29.3 [145] (γ2S splice variant) |
7.1 [146] 5.2 [168] (γ2L splice variant) 5.1 [169] (γ2L splice variant) 6.2 [125] (γ2L splice variant) |
1.7 [146] 1.9 [168] (γ2L splice variant) 1.9 [169] (γ2L splice variant) 1.4 [125] (γ2L splice variant) |
5 [125] (γ2L splice variant) 6.0 [145] (γ2S splice variant) |
||
α1β1δ | 22 [125] | No desensitization observed [125] | 400 [125] | |||
α1β2γ2 | 29 [145] (γ2S splice variant) | 11 [171] | ||||
α1β3γ2 |
25.9 [114] 26.8 [130] |
14 [171] 11.6 [130] (γ2L splice variant) 15.5 [111] (γ2L splice variant) 15.5 [182] (γ2L splice variant) |
1.48 [111] (γ2L splice variant) 1.5 [182] (γ2L splice variant) |
0.462 [114] ([GABA] = 1 mM, γ2L splice variant) | 76.1 [114] (γ2L splice variant) | 0.46 [114] (γ2L splice variant) |
α1β3δ |
23.8 [114] 26.7 [130] |
2.8 [130] 4.4 [182] |
1.4 [182] | 1.26 [114] ([GABA] = 1 mM) | 42.8 [114] | 2.4 [114] |
α1β3ε | 24 [161] (rat α1 and β3, and human ε, in L929 cells) | 0.8 [161] (rat α1 and β3, and human ε, in L929 cells) | 0.9 [161] (rat α1 and β3, and human ε, in L929 cells) | |||
α2β3γ2 | 25 [111] (γ2L splice variant) | |||||
α3β3γ2 | 35.8 [111] (γ2L splice variant) | |||||
α4β3γ2 |
10.7 [111] (γ2L splice variant) 2.57 [113] |
1.3 [113] | 2.5 [113] ([GABA] = 100 µM) | |||
α4β3δ | 0.5 [113] | 1.3 [113] | 4.8 [113] ([GABA] = 100 µM) | |||
α5β1γ2 |
32.8 [157] (γ2L splice variant) 26 [124] (γ2L splice variant) |
1.69 [157] (γ2L splice variant) | ||||
α5β3γ2 | 22 [133] (γ2L splice variant) |
5.7 [157] (γ2L splice variant) 6 [124] (γ2L splice variant) 9.4 [111] (γ2L splice variant) |
1.54 [157] (γ2L splice variant) | 51.8 [133] (γ2L splice variant) | 0.9 [133] (γ2L splice variant) | |
α5β3γ3 | 26.9 [191] | 1.5 [191] | 1.6 [191] | |||
α5β3π | 23.8 [191] | 1.3 [191] | 1.4 [191] | |||
α6β2γ2 | 2 [171] | |||||
α6β2δ | 0.2 [171] | |||||
α6β3γ2 |
2 [171] (γ2L splice variant) 2.25 [111] (γ2L splice variant) |
1.04 [111] (γ2L splice variant) | ||||
α6β3δ | 0.3 [171] |
Roman: rat subunits; bold: human subunits; italics: bovine subunits. The Hill coefficient, GABA EC50, main conductance state and characteristic times of activation, deactivation and desensitization of the most abundant subtypes in vivo, i.e. ternary subtypes and ρ homopentamers, are presented. Information on other subtypes can be found in [13, 103, 112, 114, 116, 123, 125, 130, 146, 152–157, 176, 180, 182, 191, 192]