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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).
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.
Tocris offers the following scientific literature for GABAA and GABAA-ρ Receptors to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.