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The gabapentinoids are 3-substituted derivatives of GABA; hence, they are GABA analogues, as well as γ-amino acids. [3] [4] Specifically, pregabalin is (S)-(+)-3-isobutyl-GABA, phenibut is 3-phenyl-GABA, [28] and gabapentin is a derivative of GABA with a cyclohexane ring at the 3 position (or, somewhat inappropriately named, 3-cyclohexyl-GABA).
Alcohol is another substance that often cross-tolerates with other drugs. Findings of cross-tolerance with nicotine in animal models suggest that it is also possible in humans, and may explain why the two drugs are often used together. [6] Numerous studies have also suggested the possibility of cross-tolerance between alcohol and cannabis. [7]
The transporter and its effect on GABA concentrations in the amygdala has been implicated as a key player in the disease of alcoholism. In studies conducted on rat populations, reduction of GAT3 caused rats who formerly preferred sugar to prefer alcohol. Further, studies of deceased alcoholics show a decreased concentration of GAT3 in their brains.
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 ...
Ethanol (alcohol) has a very similar mechanism of tolerance and withdrawal to benzodiazepines, involving the GABA A receptors, NMDA receptors and AMPA receptors, but the majority of research into kindling has primarily focused on alcohol. [6] An intensification of anxiety and other psychological symptoms of alcohol withdrawal also occurs. [10]
Gabapentin at a low dose of 100 mg has a T max (time to peak levels) of approximately 1.7 hours, while the T max increases to 3 to 4 hours at higher doses. [85] Food does not significantly affect the T max of gabapentin and increases the C max and area-under-curve levels of gabapentin by approximately 10%. [93]
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 ionotropic GABA A receptor protein complex is also the molecular target of the benzodiazepine class of tranquilizer drugs. Benzodiazepines do not bind to the same receptor site on the protein complex as does the endogenous ligand GABA (whose binding site is located between α- and β-subunits), but bind to distinct benzodiazepine binding sites situated at the interface between the α- and ...