Table 1 Point mutations in β2 and γ2 used in this study.
From: α subunits in GABAA receptors are dispensable for GABA and diazepam action
mutation | effect in α1β2γ2 | homologous residues in α1 or β2 | effect of homologous mutations in α1β2γ2 | Lit. |
|---|---|---|---|---|
β2Y62L | 30-fold decrease in EC50 GABA | α1F64L | 200-fold decrease in EC50 GABA | |
no shift in antagonist apparent affinity | 200-fold decrease in antagonist apparent affinity | |||
β2T202S | 20-fold decrease in EC50 GABA | (α1T206C) | (5-fold increase in EC50 GABA) | |
(no effect on DZ affinity) | ||||
(α1T206V) | (7-fold decrease in DZ affinity) | |||
γ2F77Y | 230-fold decrease in DZ affinity | |||
no effect on EC50 GABA | ||||
γ2S217A | Not available | (β2T202A) | (drastic loss of EC50 GABA) | |
(α1T206A) | (3-fold decrease in DZ affinity) | |||
γ2Y220Q | Not available | α1Y209Q | see above |
