Gamma-aminobutyric acid (GABA) is the primary inhibitory neurotransmitter in the central nervous system, causing a hyperpolarization of the membrane through the opening of a Cl- channel associated with the GABAA receptor (GABAA-R) subtype. GABAA-Rs are important therapeutic targets for a range of sedative, anxiolytic, and hypnotic agents and are implicated in several diseases including epilepsy, anxiety, depression, and substance abuse. The GABAA-R is a multimeric subunit complex. To date six α's, four β's, and four γ's, plus alternative splicing variants of some of these subunits, have been identified. Injection in oocytes or mammalian cell lines of cRNA coding for α and β subunits results in the expression of functional GABAA-Rs sensitive to GABA. However, co-expression of a γ subunit is required for benzodiazepine modulation. The various effects of the benzodiazepines in brain may also be mediated via different α subunits of the receptor. More recently there have been a number of studies demonstrating that the δ subunit of the receptor may affect subunit assembly and may also confer differential sensitivity to neurosteroids and to ethanol.WARNING This product is not for human or veterinary use.
