International Union of Pharmacology. LXX. Subtypes of γ-Aminobutyric Acid_AReceptors: Classification on the Basis of Subunit Composition, Pharmacology, and Function. Update

Increased GABAA channel subunits expression in CD8+ but not in CD4+ T cells in BB rats developing diabetes compared to their congenic littermates

“…The exception is channels formed by thesubunits, they can be homomeric. The pharmacological and functional properties are defined by the subunit composition of the channels and can be influenced by intracellular accessory proteins (Birnir and Korpi, 2007;Olsen and Sieghart, 2008). Wild-type DR +/+ rats are neither lymphopenic nor develop T1D spontaneously whereas the DR lyp/lyp rats are lymphopenic and develop T1D spontaneously varies between the cell types and also between DR lyp/lyp and DR +/+ animals.…”

“…Delta is a prominent subunit in neural extrasynaptic-type GABA A channels and makes the channels highly sensitive to the steroid THDOC. 4 and 6 subunits are also associated with extrasynaptic channels and are thought to form high-affinity (nM-low M) GABA A channels (Olsen and Sieghart, 2008). The other GABA A channel subunits present can be either associated with extrasynaptic or synaptic-like channels.…”

“…Outside the nervous system GABA is produced by the pancreatic islet  cells and is present in blood in low concentrations. Pancreatic  cells and some blood cells express GABA A channels (Gladkevich et al, 2006;Olsen and Sieghart, 2008). In T lymphocytes it is known that neurotransmitters´ receptors can be regulated by the T cell receptor activation, cytokines or the neurotransmitters themselves (Bjurstom et al, 2008; have in normal T cell function and disease.…”

HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen (Sophora flavescens root)

“…Up to now 19 different subunit isoforms have been identified in the human genome and form GABA A receptors in numerous combinations [1]. The most abundant GABA A receptor subtype is composed of 2α 1 , 2β 2 , and 1γ 2 subunits. More than 10 subtypes composed of other subunit combinations have been identified [2], which differ in tissue localization, functional characteristics, and pharmacological properties [3,4].…”

“…The most abundant GABA A receptor subtype is composed of 2α 1 , 2β 2 , and 1γ 2 subunits. More than 10 subtypes composed of other subunit combinations have been identified [2], which differ in tissue localization, functional characteristics, and pharmacological properties [3,4]. GABA A receptors possess several binding sites for small molecules, and are target for numerous drugs used to treat anxiety, panic, insomnia, and epilepsy [5,6].…”