Target type: biologicalprocess
The directed movement of gamma-aminobutyric acid (GABA, 4-aminobutyrate) into a cell or organelle. [GOC:ai]
Gamma-aminobutyric acid (GABA) import is a crucial process for maintaining neuronal function and neurotransmission. It involves the movement of GABA across the cell membrane, primarily into neurons and glial cells, via specific transporter proteins.
The process begins with GABA binding to the transporter protein on the cell membrane. This binding triggers a conformational change in the protein, opening a channel that allows GABA to move from the extracellular space into the cell.
There are two major classes of GABA transporters:
- **GAT-1 (SLC6A1)**: This is the most abundant GABA transporter in the brain, primarily localized on neurons and glial cells. GAT-1 is responsible for the majority of GABA uptake and plays a critical role in regulating synaptic GABA levels.
- **GAT-3 (SLC6A11)**: Found on neurons, GAT-3 contributes to GABA uptake and is involved in regulating GABA levels in specific brain regions.
The import of GABA is a highly regulated process influenced by several factors:
- **Concentration gradient:** GABA moves from an area of high concentration outside the cell to an area of low concentration inside the cell.
- **Membrane potential:** The electrochemical gradient across the cell membrane influences GABA transport.
- **Modulators:** Several molecules can modulate GABA transporter activity, including neurosteroids, benzodiazepines, and certain drugs.
GABA import has significant implications for:
- **Neurotransmission:** By regulating GABA levels in the synapse, transporters play a critical role in controlling inhibitory neurotransmission, which is essential for brain function.
- **Glial function:** GABA uptake by glial cells is important for buffering extracellular GABA levels and regulating neuronal excitability.
- **Pathology:** Dysregulation of GABA transport is implicated in various neurological disorders, including epilepsy, anxiety, and schizophrenia.
Understanding the mechanisms of GABA import is crucial for developing new therapeutic approaches for treating these conditions.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Sodium- and chloride-dependent GABA transporter 2 | A sodium- and chloride-dependent GABA transporter 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NSD5] | Homo sapiens (human) |
| Sodium- and chloride-dependent taurine transporter | A sodium- and chloride-dependent taurine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:P31641] | Homo sapiens (human) |
| Sodium- and chloride-dependent GABA transporter 1 | A sodium- and chloride-dependent GABA transporter 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P30531] | Homo sapiens (human) |
| Na(+)/H(+) exchange regulatory cofactor NHE-RF1 | A Na(+)/H(+) exchange regulatory cofactor NHE-RF1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:O14745] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| gamma-aminobutyric acid | gamma-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 |
| beta-alanine | amino acid zwitterion; beta-amino acid | agonist; fundamental metabolite; human metabolite; inhibitor; neurotransmitter | |
| 2,3-diaminopropionic acid | 3-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 |
| taurine | amino sulfonic acid; zwitterion | antioxidant; Escherichia coli metabolite; glycine receptor agonist; human metabolite; mouse metabolite; nutrient; radical scavenger; Saccharomyces cerevisiae metabolite | |
| guvacine | guvacine : 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 acid | nipecotic 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 | |
| tiagabine | tiagabine : 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 |
| tiagabine hydrochloride | tiagabine hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of tiagabine and hydrogen chloride. A GABA reuptake inhibitor, it is used for the treatment of epilepsy. | hydrochloride | anticonvulsant; GABA reuptake inhibitor |
| n-(4,4-diphenyl-3-butenyl)nipecotic acid | N-(4,4-diphenyl-3-butenyl)nipecotic acid: structure given in first source | diarylmethane | |
| nnc 711 | NNC 711: structure in first source | ||
| sk&f 100330-a | SK&F 100330-A: structure given in first source | ||
| ci 966 | CI 966: GABA uptake blocker; RN from Toxlit | diarylmethane | |
| hinokinin | hinokinin : A lignan that is dihydrofuran-2(3H)-one (gamma-butyrolactone) substituted by a 3,4-methylenedioxybenzyl group at positions 3 and 4 (the 3R,4R-diastereoisomer). hinokinin: suppresses expression of both HBsAg and HBeAg | benzodioxoles; gamma-lactone; lignan | trypanocidal drug |
| n-(1-benzyl-4-piperidinyl)-2,4-dichlorobenzamide | N-(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 | |
| fh535 | FH535: inhibits Wnt signaling | sulfonamide | |
| nipecotic acid, (s)-isomer | (S)-nipecotic acid : The (S)-enantiomer of nipecotic acid. | nipecotic acid | |
| 2-ethoxy-N-[1-(phenylmethyl)-4-piperidinyl]benzamide | piperidines | ||
| nnc 05-2090 | NNC 05-2090: structure given in first source | carbazoles | |
| snap 5114 |