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The GABA A receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified into α (1–6), β (1–3), γ (1–3), δ, ε, π, θ, and ρ (1−3). The function of the receptor is different according to how the pentameric complex is put together.
The ionotropic GABA A receptor protein complex is also the molecular target of the benzodiazepine class of tranquilizer drugs. Benzodiazepines do not bind to the same receptor site on the protein complex as does the endogenous ligand GABA (whose binding site is located between α- and β-subunits), but bind to distinct benzodiazepine binding sites situated at the interface between the α- and ...
A subclass of ionotropic GABA receptors, insensitive to typical allosteric modulators of GABA A receptor channels such as benzodiazepines and barbiturates, [27] [28] [29] was designated GABA ะก receptor. [30] [31] Native responses of the GABA C receptor type occur in retinal bipolar or horizontal cells across vertebrate species. [32] [33] [34] [35]
A GABA A receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABA A receptor, a ligand-gated ion channel of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA). [1] [2] They are closely related and similar to GABA A receptor antagonists.
GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified. [6]
56486 Ensembl ENSG00000170296 ENSMUSG00000018567 UniProt O95166 Q9DCD6 RefSeq (mRNA) NM_007278 NM_019749 RefSeq (protein) NP_009209 NP_062723 Location (UCSC) Chr 17: 7.24 – 7.24 Mb Chr 11: 69.88 – 69.89 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Gamma-aminobutyric acid receptor-associated protein is a protein that in humans is encoded by the GABARAP gene. Function Gamma ...
Gamma-aminobutyric acid, a GABA-B receptor agonist. A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. [1] There are three receptors of the gamma-aminobutyric acid. The ...
A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activity in a positive, negative, or neutral direction with varying degrees of efficacy.