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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]
Pregabalin is not a GABA A or GABA B receptor agonist. N-Type Voltage-gated calcium channel. There are two drug-binding α 2 δ subunits, α 2 δ-1 and α 2 δ-2, and pregabalin shows similar affinity for (and hence lack of selectivity between) these two sites. [31]
Homotaurine has been reported as a GABA antagonist, [4] as well as a GABA agonist. [10] [11] In vitro studies have found that homotaurine is a GABA A partial agonist [12] as well as a GABA B receptor partial agonist with low efficacy, becoming an antagonist and displacing the full agonists GABA and baclofen at this receptor. [13]
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 ...
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 ...
In Italy, the gold standard for treatment of high-dose benzodiazepine dependency is 8–10 days of low-dose, slowly infused flumazenil. [26] One addiction treatment centre in Italy has used flumazenil to treat over 300 patients who were dependent on high doses of benzodiazepines (up to 70 times higher than conventionally prescribed) with ...
Alfaxalone is used as an induction agent, an injectable anesthetic, and a sedative in animals. [5] While it is commonly used in cats and dogs, it has also been successfully used in rabbits, [6] horses, sheep, pigs, and exotics such as red-eared turtles, axolotl, green iguanas, marmosets, [7] and koi fish. [8]
γ-Hydroxybutyric acid, also known as gamma-hydroxybutyric acid, GHB, or 4-hydroxybutanoic acid, is a naturally occurring neurotransmitter and a depressant drug.It is a precursor to GABA, glutamate, and glycine in certain brain areas.
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