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In pharmacology, GABA A receptor positive allosteric modulators, also known as GABAkines or GABA A receptor potentiators, [1] are positive allosteric modulator (PAM) molecules that increase the activity of the GABA A receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system.
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]
The plasma membrane GABA transporters maintain an extracellular GABA concentration in the vicinity of the synapse to control the activity of the GABA receptors. The GABAergic synaptic transmission controls the generation of membrane potential rhythmic changes as the transporters are dependent on Na + and Cl − ions moving in and out of the ...
[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.
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 ...
A GABA analogue is a compound which is an analogue or derivative of the neurotransmitter gamma-Aminobutyric acid (GABA) (the IUPAC of which is 4-aminobutanoic acid). Many GABA analogues are used as drugs , especially as anticonvulsants , sedatives , and anxiolytics .
GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified. [6]
Alcohol acts as a general central nervous system depressant, but it also affects some specific areas of the brain to a greater extent than others. Memory impairment caused by alcohol has been linked to the disruption of hippocampal function—particularly affecting gamma-Aminobutyric acid (GABA) and N-methyl-D-aspartate (NMDA) neurotransmission which negatively impacts long-term potentiation ...