Abstract: Inhibition of the central nervous system(CNS) is mainly mediated by GABAergic neurons,its nervous transmission is important for all aspects of CNS function.The effects of central GABAergic system are mainly mediated by both GABA_A receptors,which belong to the superfamily of heteropentameric ligand-gated ion channels,and GABA_B receptors,which belong to superfamily of G-protein coupled heptahelical transmembrane receptors.Fast synaptic inhibition in the mammalian brain is mainly mediated by GABA_A receptors.In this chapter,we summarized recent findings on the molecular mechanisms of intracellular transportation and functions of GABA_A receptors,and discussed the regulating roles of post-translational modifications,GABA_A receptors associated proteins,scaffold proteins,enzymes etc in this process.Finally,we highlighted a number of neuropsychical diseases, in which confusion of GABAA receptors trafficking occured.