Activation of GABAA Receptors: Views from Outside the Synaptic Cleft

Some GABA(A) receptors (GABA(A)Rs) are activated by low transmitter levels present in the extracellular space and generate an uninterrupted conductance referred to as "tonic." This tonic conductance is highly sensitive to all factors regulating the amount of GABA surrounding the neurons. Only a few GABA(A)Rs with particular subunit combinations are well suited to mediate the tonic conductance. These same receptors constitute important and specific targets for various endogenous and exogenous neuroactive compounds and possible therapeutic targets.