Glutamate Reuptake Inhibitor
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An excitatory amino acid reuptake inhibitor (EAARI) is a type of
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 insuffla ...
which inhibits the
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 transm ...
of the
excitatory In neuroscience, an excitatory postsynaptic potential (EPSP) is a postsynaptic potential that makes the postsynaptic neuron more likely to fire an action potential. This temporary depolarization of postsynaptic membrane potential, caused by the ...
neurotransmitter A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell. Neuro ...
s
glutamate Glutamic acid (symbol Glu or E; the ionic form is known as glutamate) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can syn ...
and
aspartate Aspartic acid (symbol Asp or D; the ionic form is known as aspartate), is an α-amino acid that is used in the biosynthesis of proteins. Like all other amino acids, it contains an amino group and a carboxylic acid. Its α-amino group is in the pro ...
by blocking one or more of the
excitatory amino acid transporter Glutamate transporters are a family of neurotransmitter transporter proteins that move glutamate – the principal excitatory neurotransmitter – across a membrane. The family of glutamate transporters is composed of two primary subclasses: the ex ...
s (EAATs). Examples of EAARIs include
dihydrokainic acid Dihydrokainic acid is an organic compound that contains two carboxylic acid functional groups, making it a dicarboxylic acid. It is an inhibitor of the GLT-1 glutamate transporter. See also * Kainic acid Kainic acid, or kainate, is an acid ...
(DHK) and
WAY-213,613 WAY-213,613 is a drug which acts as a reuptake inhibitor for the glutamate transporter subtype EAAT2, selective over other glutamate transporter subtypes and highly selective over metabotropic and ionotropic glutamate receptor Glutamate recep ...
, selective blockers of
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 thi ...
(GLT-1), and L-''trans''-2,4-PDC, a non-selective blocker of all five EAATs.
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 ...
is a selective noncompetitive reuptake inhibitor of presynaptic
EAAT3 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 ...
(via transporter endocytosis) in dopamine neurons. L-Theanine is reported to competitively inhibit reuptake at
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, al ...
(GLAST) and
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 thi ...
(GLT-1).


See also

*
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 transmit ...
*
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 agonist ...
*
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 increa ...
*
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-540 ...
*
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-M ...
*
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 receptors. Examples include: * AP5 * Barbiturates * Dextromethorphan * Dext ...


References


External links

* {{pharmacology-stub