GABAA (α1, β2, γ2) receptors belong to the family of fast ligand gated receptors. They are anion permeable and the ligand-induced currents show multiple sublevels. However, the pharmacology of the receptors within this family varies greatly. GABA is the primary inhibitory neurotransmitter in the mammalian CNS. Activation of GABAA (α1, β2, γ2) receptors by GABA tends to decrease neuronal excitability. |
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Ligand dependent activation of GABAA (α1, β2, γ2) receptors. Activation by 1, 3 and 10 μM GABA from a GABAA (α1, β2, γ2) expressing HEK293 cell. Activation shown enlarged (right). |
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| Ligand dependent activation and concentration dependend inhibition of GABAA (α1, β2, γ2) receptors. GABAA receptors were activated by 10 µM GABA. The activation of the GABA receptors were inhibited by increasing concentrations of the inhibitor Bicuculline. The Graph on the right shows the summary of 11 IC50. |