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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]
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. Other agents which may have GABA A receptor antagonism include the antibiotic ciprofloxacin, [1 ...
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures [10] [7] of epilepsy. It is a commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain. [11]
A GABAergic or GABAnergic agent is any chemical that modifies the effects of GABA in the body or brain. Some different classes of GABAergic drugs include agonists, antagonists, modulators, reuptake inhibitors and enzymes. [1]
Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, and generalized anxiety disorder (GAD).
Eszopiclone is classified as a nonbenzodiazepine or Z-drug and a sedative and hypnotic of the cyclopyrrolone group. [7] It is the S-stereoisomer of zopiclone. [5] [8] It works by interacting with the GABA receptors. [7] Approved for medical use in the United States in 2004, [3] eszopiclone is available as a generic medication. [5]
HRA Pharma, a Perrigo company, acquired rights to the medication nearly a decade ago with the intent to bring it over-the-counter. “It’s been a long journey,” Welgryn told Fortune earlier ...
DABA's main action is being an inhibitor of GABA transaminase, an enzyme that converts GABA back to glutamate. When the enzyme is inhibited, this conversion cannot happen, therefore, GABA levels are elevated. [1] It has also been observed that 2,4-diaminobutyric acid is a GABA reuptake inhibitor. [2] This action further elevates levels of GABA.
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