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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]
Tiagabine increases the level of γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system, by blocking the GABA transporter 1 (GAT-1), and hence is classified as a GABA reuptake inhibitor (GRI). [4] [13]
Tiagabine, a selective GABA reuptake inhibitor used as an anticonvulsant in the treatment of epilepsy and seizures. Standard reuptake inhibitors are believed to act simply as competitive substrates that work by binding directly to the plasmalemma transporter of the neurotransmitter in question.
DABA's main action is being an inhibitor of GABA transaminase, an enzyme that converts GABA back to glutamate. When the enzyme is inhibited, this conversion cannot happen, therefore, GABA levels are elevated. [1] It has also been observed that 2,4-diaminobutyric acid is a GABA reuptake inhibitor. [2] This action further elevates levels of GABA.
Pages in category "GABA reuptake inhibitors" The following 14 pages are in this category, out of 14 total. This list may not reflect recent changes. ...
SNRIs (serotonin and norepinephrine reuptake inhibitors) hit serotonin and norepinephrine. Wellbutrin (bupropion)—the only FDA-approved NDRI (norepinephrine and dopamine reuptake inhibitor) for ...
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]
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 ...