GABAA and GABAA-ρ Receptors

GABAA receptors are ligand-gated ion channels, which, along with the 7-TM GABAB receptors, are responsible for mediating the inhibitory effects of GABA. They are Cys-loop family ion channels that form a pentameric intrinsic anion channel. In mammals, 6α, 3β, 3γ, 1δ, 3ρ, 1ε, 1π and 1θ and subunits have been identified. GABAA receptors comprise mainly the α-, β- and γ-subunits, but a subgroup of GABAA receptors are formed exclusively from ρ subunits. These GABAA-ρ receptors are also known as GABAC receptors, however IUPHAR considers them to be a subtype of GABAA receptors and recommends against the use of the term GABAC (see Olsen and Sieghart, 2008).

GABAA and GABAA-ρ Receptor Target Files

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A variety of proteins associate with the large intracellular M3-M4 loop of GABAA and GABAC receptors and influence the trafficking, cell surface expression, internalization and function of the receptors. Furthermore, GABAA receptors have modulatory sites for benzodiazepines, barbiturates, neurosteroids and ethanol.

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