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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]
It also has low micromolecular affinity to GABA with a Michaelis-Menten constant of 2.5 μM, [1] and requires the presence of Cl- ions in the extracellular matrix. The GABA transporter help creates an equilibrium of GABA and will work in the reverse direction if needed to maintain the baseline concentration of GABA in the system. [1]
The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), ...
GABA B receptor agonists and positive allosteric modulators have been found to result in ICSS depression and have been found to inhibit the reinforcing effects of several drugs, including cocaine, methamphetamine, and nicotine, reversing the ICSS facilitation these drugs typically cause.
Binge drinking regimes are associated with causing an imbalance between inhibitory and excitatory amino acids and changes in monoamine release in the central nervous system, which increases neurotoxicity; this may result in cognitive impairments, psychological problems, and may cause irreversible brain damage in both adolescent and adult long-term binge drinkers.
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 ...
There are two subunits of the receptor, GABA B1 and GABA B2, [11] and these appear to assemble as obligate heterodimers in neuronal membranes by linking up by their intracellular C termini. [10] In the mammalian brain, two predominant, differentially expressed isoforms of the GABA B1 are transcribed from the Gabbr1 gene, GABA B(1a) and GABA B ...