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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]
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. Other agents which may have GABA A receptor antagonism include the antibiotic ciprofloxacin, [1 ...
A GABAergic or GABAnergic agent is any chemical that modifies the effects of GABA in the body or brain. Some different classes of GABAergic drugs include agonists, antagonists, modulators, reuptake inhibitors and enzymes. [1]
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 ...
The effect on sodium channels could be of particular relevance for seizure protection. Although topiramate does inhibit high-voltage-activated calcium channels, its relevance to clinical activity is uncertain. Effects on specific GABA-A receptor isoforms could also contribute to the antiseizure activity of the drug.
GABA B Receptors are similar in structure to and in the same receptor family with metabotropic glutamate receptors. [10] There are two subunits of the receptor, GABA B1 and GABA B2, [11] and these appear to assemble as obligate heterodimers in neuronal membranes by linking up by their intracellular C termini. [10]
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 ...
Bicuculline is a phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABA A receptors. [1] It was originally identified in 1932 in plant alkaloid extracts [2] and has been isolated from Dicentra cucullaria, Adlumia fungosa, and several Corydalis species (all in subfamily Fumarioideae, previously known as family Fumariaceae).