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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]
Inhibition of GABA transaminase enzymes reduces the degradation of GABA, leading to increased neuronal GABA concentrations. Examples include valproic acid , [ 2 ] vigabatrin , [ 3 ] [ 4 ] phenylethylidenehydrazine (and drugs that metabolize to it, such as phenelzine [ 5 ] ), ethanolamine- O -sulfate (EOS), and L- cycloserine .
To test whether somatosensation, specifically pain, was subjected to inhibition, scientists injected a chemical into the spinal cord of a rodent to block the primary inhibitory neurotransmitter's activity (bicuculline, a GABA receptor agonist [4]). They found that pharmacologically blocking GABA receptors actually enhanced the perception of ...
[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.
[36] [37] [38] Although the term "GABA С receptor" is frequently used, GABA С may be viewed as a variant within the GABA A receptor family. [7] Others have argued that the differences between GABA С and GABA A receptors are large enough to justify maintaining the distinction between these two subclasses of GABA receptors.
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.
GABA is also the primary inhibitory neurotransmitter in the cerebral cortex and has the highest level of expression within it. [15] The GABA affinity (K m) of the mouse isoform of GAT1 is 8 μM. [16] In the brain of a mature mammal, glutamate is converted to GABA by the enzyme glutamate decarboxylase (GAD) along with the addition of vitamin B6.
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 ...