Propofol acts upon the GABAa receptors, causing it's activation, similarly to [[#barbituates|thiopental]], although it binds at a different site. This causes increased chloride conductance leading to hyperpolarisation.
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Propofol binds to and activates GABA-A receptors, similarly to [[#barbituates|thiopental]], benzodiazepines and alcohol, although it binds at a different site on this complex multi-subunit receptor. GABA is a major inhibitory neurotransmitter in the CNS. Activation of the GABA-A receptor causes increased chloride conductance leading to hyperpolarisation of the postsynaptic neuronal cell membrane, thus inhibiting conductance producing depression of the CNS.