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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]
Gabaculine is a naturally occurring neurotoxin first isolated from the bacteria Streptomyces toyacaensis, [1] which acts as a potent and irreversible GABA transaminase inhibitor, [2] [3] and also a GABA reuptake inhibitor. [4] [5] Gabaculine is also known as 3-amino-2,3-dihydrobenzoic acid hydrochloride [6] and 5-amino cyclohexa-1,3 dienyl ...
Like other GABA-T inhibitors, γ-acetylenic GABA causes GABA levels in the brain to be elevated. This is due to 4-aminobutyrate transaminase being the enzyme that converts γ-aminobutyric acid to L-glutamate. Inhibiting the enzyme stops this conversion from happening.
GABA acts via binding to its receptors which include the ligand gated ion channels, GABA A and GABA C and the G-protein couple receptors GABA B. The GABA B receptor has been found to be the most important of the three receptors for this disorder as it is vital in both GABA and GHB release.
Vigabatrin reduced cholecystokinin tetrapeptide-induced symptoms of panic disorder, in addition to elevated cortisol and ACTH levels, in healthy volunteers. [12]Vigabatrin is also used to treat seizures in succinic semialdehyde dehydrogenase deficiency (SSADHD), which is an inborn GABA metabolism defect that causes intellectual disability, hypotonia, seizures, speech disturbance, and ataxia ...
[9] [10] Because GABA-T degrades GABA, the inhibition of this enzyme has been the target of many medical studies. [9] The goal of these studies is to find a way to inhibit GABA-T activity, which would reduce the rate that GABA and 2-oxoglutarate are converted to semialdehyde and L-glutamate, thus raising GABA concentration in the brain.
The gabapentinoids are 3-substituted derivatives of GABA; hence, they are GABA analogues, as well as γ-amino acids. [ 3 ] [ 4 ] Specifically, pregabalin is ( S )-(+)-3-isobutyl-GABA, phenibut is 3-phenyl-GABA, [ 28 ] and gabapentin is a derivative of GABA with a cyclohexane ring at the 3 position (or, somewhat inappropriately named, 3 ...
GABRA2 is an alpha subunit that is part of GABA-A receptors, which are ligand-gated chloride channels and are activated by the major inhibitory neurotransmitter in the mammalian brain, GABA. Chloride conductance of these channels can be modulated by agents, such as benzodiazepines (psychoactive drugs) that bind to the GABA-A receptor.