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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 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]
Because GABA is integral to the release of inhibitory neurotransmitters which produce a calming effect and play a role in reducing anxiety, stress, and fear, it is not surprising that polymorphisms in these genes result in more consequences relating to mental health than to physical health.
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.
Darigabat (developmental code names CVL-865, PF-06372865, PF-6372865) is a GABAergic medication which is under development for the treatment of photosensitive epilepsy, focal onset seizures, panic disorder, and other anxiety disorders.
Gaboxadol is a supra-maximal agonist at α 4 β 3 δ, low-potency agonist at α 1 β 3 γ 2, partial agonist at α 4 β 3 γ, and antagonist at ρ1 GABA A receptors. [5] [6] [7] Its affinity for extrasynaptic α 4 β 3 δ GABA A receptors is 10-fold greater than other subtypes. [8]