How Much GABA Is Needed to Evoke a Response

The cloning of GABAa and GABAb receptors has enabled researchers to study the properties of receptors of known covalent structure. In most of these in vitro studies, the KD of the cloned receptors for GABA is in the micromolar range, but in vivo GABA often has an EC50 in the nanomolar or even subnanomolar range.

Within a synaptic cleft, the concentration of GABA is estimated to be in the millimolar range, enough to saturate postsynaptic GABAa (and GABAb)

receptors. The occurrence of GABAa and GABAB receptors outside of synapses suggests that GABA may also act outside of synapses. The ability of cultured cells and partially purified receptors to bind GABA at nanomolar concentrations is consistent with a role for nonsynaptic GABA, particularly in response to injury, seizures, and other stresses.

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