An excitatory amino acid reuptake inhibitor (EAARI) is a type of
drug 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 Synapse, pre-synaptic neuron at a synapse) or glial cell after it has performed its function of ...
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 ...
neurotransmitters
glutamate and
aspartate 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 (DHK) and
WAY-213,613, 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.
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
E ...
(via transporter endocytosis) in dopamine neurons.
is reported to competitively inhibit reuptake at
EAAT1 (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 transmi ...
*
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 agonis ...
*
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 incre ...
*
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, AL ...
*
Excitatory amino acid receptor agonist An excitatory amino acid receptor agonist, or glutamate receptor agonist, is a chemical substance which agonizes one or more of the glutamate receptors.
Examples include:
* AMPA
* Glutamic acid
* Ibotenic acid
* Kainic acid
* ''N''-Methyl-D-asp ...
*
Excitatory amino acid receptor antagonist An excitatory amino acid receptor antagonist, or glutamate receptor antagonist, is a chemical substance which antagonizes one or more of the glutamate receptors.
Examples include:
* AP5
* Barbiturates
* Dextromethorphan
* Dextrorphan
* Dizocilpin ...
References
External links
*
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