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gamma-aminobutyric acid transport

Definition

Target type: biologicalprocess

The directed movement of gamma-aminobutyric acid (GABA, 4-aminobutyrate), an amino acid which acts as a neurotransmitter in some organisms, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:go_curators, ISBN:0198506732]

Gamma-aminobutyric acid (GABA) transport is a crucial biological process that regulates the concentration of GABA, a major inhibitory neurotransmitter in the central nervous system. This transport involves the movement of GABA across cell membranes, primarily via specialized transporter proteins.

There are two main types of GABA transporters:

1. **Plasma membrane GABA transporters (GATs):** These proteins are responsible for the uptake of GABA from the synaptic cleft, the space between neurons where neurotransmission occurs. GATs are responsible for terminating GABA signaling by removing GABA from the synapse, thus ensuring efficient and precise neuronal communication.

2. **GABA transporter proteins in glial cells:** Astrocytes, a type of glial cell in the brain, also express GABA transporters. These transporters play a critical role in regulating GABA levels in the extracellular space and may contribute to the recycling of GABA for neuronal reuptake.

**Mechanism of GABA transport:**

GABA transport is an active process, meaning it requires energy to move GABA against its concentration gradient. This energy is typically derived from the hydrolysis of ATP, which is the main energy currency of cells.

GABA transporters operate via a secondary active transport mechanism, often coupled with the movement of sodium ions (Na+) down their concentration gradient. This means that the energy stored in the electrochemical gradient of Na+ is used to power the movement of GABA into the cell.

**Specific GABA transporters and their functions:**

* **GAT-1:** This transporter is the most abundant GABA transporter in the brain and is responsible for the majority of GABA uptake from the synapse. GAT-1 is found on both neurons and glial cells.

* **GAT-2:** This transporter is primarily expressed in glial cells and plays a role in the regulation of GABA levels in the extracellular space.

* **GAT-3:** This transporter is found in both neurons and glial cells and is involved in the uptake of GABA from the synapse, although it is less efficient than GAT-1.

* **GAT-4:** This transporter is primarily expressed in the periphery and is involved in the uptake of GABA in non-neuronal tissues.

**Clinical significance:**

Dysregulation of GABA transport has been implicated in a variety of neurological disorders, including epilepsy, anxiety, and depression. Medications targeting GABA transporters are being developed to treat these conditions by modulating GABA levels in the brain.

**In summary, GABA transport is a critical process for regulating GABA levels in the brain and ensuring efficient neuronal communication. The process is mediated by specialized transporter proteins located on both neurons and glial cells. Dysregulation of GABA transport can lead to neurological disorders, highlighting its importance in maintaining brain health.**'
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Proteins (2)

ProteinDefinitionTaxonomy
Sodium- and chloride-dependent betaine transporterA sodium- and chloride-dependent betaine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48065]Homo sapiens (human)
Sodium- and chloride-dependent creatine transporter 1A sodium- and chloride-dependent creatine transporter 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48029]Homo sapiens (human)

Compounds (13)

CompoundDefinitionClassesRoles
gamma-aminobutyric acidgamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.

gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.
amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid
human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
2,3-diaminopropionic acid3-aminoalanine : A diamino acid that is alanine in which one of the hydrogens of the methyl group is replaced by an amino group.alanine derivative;
amino acid zwitterion;
beta-amino acid;
diamino acid;
non-proteinogenic alpha-amino acid
Escherichia coli metabolite
creatineglycine derivative;
guanidines;
zwitterion
geroprotector;
human metabolite;
mouse metabolite;
neuroprotective agent;
nutraceutical
guvacineguvacine : A alpha,beta-unsaturated monocarboxylic acid that is nicotinic acid which has been hydrogenated at the 1-2 and 5-6 positions of the pyridine ring.

guvacine: RN given refers to parent cpd
alpha,beta-unsaturated monocarboxylic acid;
beta-amino acid;
pyridine alkaloid;
secondary amino compound;
tetrahydropyridine
GABA reuptake inhibitor;
plant metabolite
nipecotic acidnipecotic acid : A piperidinemonocarboxylic acid that is piperidine in which one of the hydrogens at position 3 is substituted by a carboxylic acid group.

nipecotic acid: RN given refers to cpd without isomeric designation
beta-amino acid;
piperidinemonocarboxylic acid
tiagabinetiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy.

Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.
beta-amino acid;
piperidinemonocarboxylic acid;
tertiary amino compound;
thiophenes
anticonvulsant;
GABA reuptake inhibitor
ci 966CI 966: GABA uptake blocker; RN from Toxlitdiarylmethane
n-(1-benzyl-4-piperidinyl)-2,4-dichlorobenzamideN-(1-benzyl-4-piperidinyl)-2,4-dichlorobenzamide: inhibits the betaine-GABA transporter 1; structure in first source
nipecotic acid(R)-nipecotic acid : The (R)-enantiopmer of nipecotic acid.amino acid zwitterion;
nipecotic acid
nipecotic acid, (s)-isomer(S)-nipecotic acid : The (S)-enantiomer of nipecotic acid.nipecotic acid
2-ethoxy-N-[1-(phenylmethyl)-4-piperidinyl]benzamidepiperidines
nnc 05-2090NNC 05-2090: structure given in first sourcecarbazoles
snap 5114