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The subset of GABA A receptors that also bind benzodiazepines are referred to as benzodiazepine receptors (BzR). The GABA A receptor is a heteromer composed of five subunits, the most common ones being two αs, two βs, and one γ (α 2 β 2 γ1). For each subunit, many subtypes exist (α 1–6, β 1–3, and γ 1–3).
GABA receptor antagonists are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant effects, and are mainly used for counteracting overdoses of sedative drugs. Examples include bicuculline, securinine and metrazol, and the benzodiazepine GABA A receptor antagonist flumazenil.
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]
In vitro studies of tissue cultured cell lines have shown that chronic treatment with flumazenil enhanced the benzodiazepine binding site where such receptors have become more numerous and uncoupling/down-regulation of GABA A has been reversed. [19] [20] [21] After long-term exposure to benzodiazepines, GABA A receptors become down-regulated ...
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 ...
For receptor level, the traditional antidotes include naloxone and flumazenil. Flumazenil functions as a competitive antagonist at the GABA-A receptor complex's benzodiazepine site. By doing this, the CNS and respiratory depression would reverse and the inward chloride current would reduce.
A GABA reuptake inhibitor (GRI) is a type of drug which acts as a reuptake inhibitor for the neurotransmitter gamma-Aminobutyric acid (GABA) by blocking the action of the gamma-Aminobutyric acid transporters (GATs). This in turn leads to increased extracellular concentrations of GABA and therefore an increase in GABAergic neurotransmission. [1]