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GABAA and GABAA-ρ receptors are ligand-gated ion channels, which, along with the G-protein coupled GABAB receptors, mediate the effects of GABA. GABA is the major inhibitory neurotransmitter in the central nervous system and is present in interneurons and projection neurons throughout the brain, and also plays important roles in the peripharal nervous system.
GABAA receptors are formed from five subunits and are permeable to Cl- ions and, to a lesser extent, bicarbonate ions (HCO-). These receptors have extremely complex pharmacological profiles due to the presence of multiple subtypes of each subunit, splice variants of those subtypes and specific binding sites for multiple different compound classes. The specificity of individual ligands is determined by the subunit conformation of a single receptor.
In mammals there are 8 subunit families, some of which have multiple subtpes; 6α, 3β, 3γ, 1δ, 3ρ, 1ε, 1π and 1θ. The majority of endogenous GABAA receptors in the human brain are composed of two α-subunits, two β-subunits and a single γ-subunit. A subclass of GABAA receptors, GABAA-ρ receptors, are homomeric channels formed exclusively from ρ-subunits. These receptors were previously known as GABAC receptors.
All GABAA subunits have a similar structure with a long N-terminal extracellular domain, four a-helical transmembrane domains (M1 to M4) and a long intracellular loop between M3 and M4. A variety of proteins associate with the large intracellular M3-M4 loop of GABAA and GABAA-ρ receptors and influence the trafficking, cell surface expression, internalization and function of the receptors. For example, the M3/M4 loop contains a phosphorylation site for Protein Kinase C in the majority of GABAA receptor subunits; the presence of this phosphorylation site is splice variant-dependent.
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.