Glutamate Reuptake Inhibitor
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Glutamate Reuptake Inhibitor
An excitatory amino acid reuptake inhibitor (EAARI) is a type of drug which inhibits the reuptake of the excitatory neurotransmitters glutamate and aspartate by blocking one or more of the excitatory amino acid transporters (EAATs). Examples of EAARIs include dihydrokainic acid (DHK) and WAY-213,613, selective blockers of EAAT2 (GLT-1), and L-''trans''-2,4-PDC, a non-selective blocker of all five EAATs. Amphetamine is a selective noncompetitive reuptake inhibitor of presynaptic EAAT3 (via transporter endocytosis) in dopamine neurons. L-Theanine is reported to competitively inhibit reuptake at EAAT1 (GLAST) and EAAT2 (GLT-1). See also * Reuptake inhibitor * Glutamatergic * GABA reuptake inhibitor * Glycine reuptake inhibitor * Excitatory amino acid receptor agonist * Excitatory amino acid receptor antagonist An excitatory amino acid receptor antagonist, or glutamate receptor antagonist, is a chemical substance which Receptor antagonist, antagonizes one or more of the glutamate rec ...
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Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ...
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SLC1A1
Excitatory amino acid transporter 3 (EAAT3), is a protein that in humans is encoded by the ''SLC1A1'' gene. Tissue distribution EAAT3 is expressed on the plasma membrane of neurons, specifically on the dendrites and axon terminals. Function Excitatory amino acid transporter 3 is a member of the high-affinity glutamate transporters which plays an essential role in transporting glutamate across plasma membranes in neurons. In the brain, excitatory amino acid transporters are crucial in terminating the postsynaptic action of the neurotransmitter glutamate, and in maintaining extracellular glutamate concentrations below neurotoxic levels. EAAT3 also transports aspartate, and mutations in this gene are thought to cause dicarboxylic aminoaciduria, also known as glutamate-aspartate transport defect. EAAT3 is also the major route of neuronal cysteine uptake. Cysteine is a component of the major antioxidant glutathione, and mice lacking EAAT3 exhibit reduced levels of glutathione in ...
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Excitatory Amino Acid Receptor Agonist
An excitatory amino acid receptor agonist, or glutamate receptor agonist, is a chemical substance which receptor agonist, agonizes one or more of the glutamate receptors. Examples include: * AMPA * Glutamic acid * Ibotenic acid * Kainic acid * N-Methyl-D-aspartic acid, ''N''-Methyl-D-aspartic acid * Quisqualic acid See also * Excitatory amino acid receptor antagonist * Excitatory amino acid reuptake inhibitor References External links

* Amino acids Excitatory amino acid receptor agonists, {{nervous-system-drug-stub ...
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Glycine Reuptake Inhibitor
A glycine reuptake inhibitor (GRI) is a type of drug which inhibits the reuptake of the neurotransmitter glycine by blocking one or more of the glycine transporters (GlyTs). Examples of GRIs include bitopertin (RG1678), Org 24598, Org 25935, ALX-5407, and sarcosine, which are selective glycine transporter 1, GlyT1 transporter blocker, blockers, and Org 25543 and N-arachidonylglycine, which are selective glycine transporter 2, GlyT2 blockers. Some weak and/or non-selective GlyT blockers include amoxapine and ethanol (alcoholic beverage, alcohol). See also * Reuptake inhibitor * Glycinergic * GABA reuptake inhibitor * Excitatory amino acid reuptake inhibitor References

Glycine reuptake inhibitors {{nervous-system-drug-stub ...
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GABA Reuptake Inhibitor
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. Indications GRIs may be used in the clinical treatment of seizures, convulsions, or epilepsy as anticonvulsants/antiepileptics, anxiety disorders such as generalized anxiety disorder (GAD), social phobia (SP) also known as social anxiety disorder (SAD), and panic disorder (PD) as anxiolytics, insomnia as hypnotics, muscle tremors or spasms as muscle relaxants, and chronic pain as analgesics. They may also potentially be used as anesthetics in surgery. Effects GRIs can induce a wide range of psychological and physiological effects, including: * general and subjective alteration in consciousness * dizziness * blurry vision * diplopia or ...
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Glutamatergic
Glutamatergic means "related to glutamate". A glutamatergic agent (or drug) is a chemical that directly modulates the excitatory amino acid (glutamate/ aspartate) system in the body or brain. Examples include excitatory amino acid receptor agonists, excitatory amino acid receptor antagonists, and excitatory amino acid reuptake inhibitors. See also * Adenosinergic * Adrenergic * Cannabinoidergic * Cholinergic * Dopaminergic * GABAergic * GHBergic * Glycinergic * Histaminergic * Melatonergic * Monoaminergic * Opioidergic * Serotonergic * Sigmaergic Sigma receptors (σ-receptors) are protein cell surface receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine, and siramesine. There are two subtypes, ... References Neurochemistry Neurotransmitters {{nervous-system-drug-stub ...
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Reuptake Inhibitor
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmitting a neural impulse. Reuptake is necessary for normal synaptic physiology because it allows for the recycling of neurotransmitters and regulates the level of neurotransmitter present in the synapse, thereby controlling how long a signal resulting from neurotransmitter release lasts. Because neurotransmitters are too large and hydrophilic to diffuse through the membrane, specific transport proteins are necessary for the reabsorption of neurotransmitters. Much research, both biochemical and structural, has been performed to obtain clues about the mechanism of reuptake. Protein structure The first primary sequence of a reuptake protein was published in 1990. The technique for protein sequence determination relied upon the purification, se ...
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EAAT2
Excitatory amino acid transporter 2 (EAAT2) also known as solute carrier family 1 member 2 (SLC1A2) and glutamate transporter 1 (GLT-1) is a protein that in humans is encoded by the ''SLC1A2'' gene. Alternatively spliced transcript variants of this gene have been described, but their full-length nature is not known. Function SLC1A2 / EAAT2 is a member of a family of the solute carrier family of proteins. The membrane-bound protein is the principal transporter that clears the excitatory neurotransmitter glutamate from the extracellular space at synapses in the central nervous system. Glutamate clearance is necessary for proper synaptic activation and to prevent neuronal damage from excessive activation of glutamate receptors. EAAT2 is responsible for over 90% of glutamate reuptake within the brain. Clinical significance Mutations in and decreased expression of this protein are associated with amyotrophic lateral sclerosis (ALS). The drug riluzole approved for the treatment ...
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EAAT1
Excitatory amino acid transporter 1 (EAAT1) is a protein that, in humans, is encoded by the ''SLC1A3'' gene. EAAT1 is also often called the GLutamate ASpartate Transporter 1 (GLAST-1). EAAT1 is predominantly expressed in the plasma membrane, allowing it to remove glutamate from the extracellular space. It has also been localized in the inner mitochondrial membrane as part of the malate-aspartate shuttle. Mechanism EAAT1 functions ''in vivo'' as a homotrimer. EAAT1 mediates the transport of glutamic acid, glutamic and aspartic acid with the Co-transport, cotransport of three sodium, Na+ and one proton, H+ ion, cations and counter transport of one potassium, K+ cation. This co-transport coupling (or symport) allows the transport of glutamate into cells against a concentration gradient. Tissue distribution EAAT1 is expressed throughout the Central nervous system, CNS, and is highly expressed in astrocytes and Bergmann glia in the cerebellum. In the retina, EAAT1 is expr ...
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Theanine
Theanine , also known as L-γ-glutamylethylamide and ''N''5-ethyl-L-glutamine, is an amino acid analogue of the proteinogenic amino acids L-glutamate and L-glutamine and is found primarily in particular plant and fungal species. It was discovered as a constituent of green tea in 1949; in 1950, it was isolated from gyokuro leaves. Theanine provides a unique brothy or savory (umami) flavor to green tea infusions. The name "theanine" without a prefix generally implies the enantiomer L-theanine, which is the form found in tea leaves and as a dietary supplement ingredient. Most studies have used L-theanine. The opposite enantiomer, D-theanine, has been studied less. The regulatory status of theanine varies by country. In Japan, L-theanine has been approved for use in all foods, with some restrictions in the case of infant foods.Sakato,Y. J. Agri. Chem. Soc. 1949, 23, 262–267 In the United States, the Food and Drug Administration (FDA) considers it to be generally recognized ...
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Amphetamine
Amphetamine (contracted from alpha- methylphenethylamine) is a strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. It is also commonly used as a recreational drug. Amphetamine was discovered in 1887 and exists as two enantiomers: levoamphetamine and dextroamphetamine. ''Amphetamine'' properly refers to a specific chemical, the racemic free base, which is equal parts of the two enantiomers in their pure amine forms. The term is frequently used informally to refer to any combination of the enantiomers, or to either of them alone. Historically, it has been used to treat nasal congestion and depression. Amphetamine is also used as an athletic performance enhancer and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant. It is a prescription drug in many countries, and unauthorized possession and distribution of amphetamine are often tightly controlled due to ...
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Reuptake
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmitting a neural impulse. Reuptake is necessary for normal synaptic physiology because it allows for the recycling of neurotransmitters and regulates the level of neurotransmitter present in the synapse, thereby controlling how long a signal resulting from neurotransmitter release lasts. Because neurotransmitters are too large and hydrophilic to diffuse through the membrane, specific transport proteins are necessary for the reabsorption of neurotransmitters. Much research, both biochemical and structural, has been performed to obtain clues about the mechanism of reuptake. Protein structure The first primary sequence of a reuptake protein was published in 1990. The technique for protein sequence determination relied upon the purification, ...
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