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Gabapentin is a 3,3-disubstituted derivative of GABA. Therefore, it is a GABA analogue, as well as a γ-amino acid. [99] [100] Specifically, it is a derivative of GABA with a pentyl disubstitution at 3 position, hence, the name - gabapentin, in such a way as to form a six-membered ring.
Because of its short elimination half-life, gabapentin must be administered 3 to 4 times per day to maintain therapeutic levels. [25] Similarly, pregabalin has been given 2 to 3 times per day in clinical studies. [24] Phenibut, also, is taken 3 times per day.
γ-Acetylenic GABA, also known as 4-aminohex-5-ynoic acid is a potent and irreversible inhibitor of GABA-T. [3] Mechanism of action
GABA (gamma-aminobutyric acid) is a neurotransmitter, or chemical messenger, in the brain that helps block signals sent out by the nervous system, which, in turn, produces a sense of calm.
The subset of GABA A receptors that also bind benzodiazepines are referred to as benzodiazepine receptors (BzR). The GABA A receptor is a heteromer composed of five subunits, the most common ones being two αs, two βs, and one γ (α 2 β 2 γ1). For each subunit, many subtypes exist (α 1–6, β 1–3, and γ 1–3).
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]
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