Target type: molecularfunction
Enables the transfer of gamma-aminobutyric acid from one side of a membrane to the other. Gamma-aminobutyric acid is 4-aminobutyrate (GABA). [GOC:go_curators, GOC:mtg_transport, ISBN:0198506732, ISBN:0815340729]
Gamma-aminobutyric acid (GABA) transmembrane transporter activity involves the movement of GABA across cell membranes. GABA is a neurotransmitter that plays a crucial role in inhibiting neuronal activity in the central nervous system. GABA transporters, also known as GABAergic transporters, are integral membrane proteins responsible for the reuptake of GABA from the synaptic cleft, the space between neurons where neurotransmission occurs. This reuptake process terminates GABA signaling and ensures efficient neurotransmission. GABA transporters are highly selective for GABA and utilize the energy from the electrochemical gradient of sodium ions (Na+) to transport GABA against its concentration gradient. The transport cycle involves several steps: 1. Binding of GABA and Na+ ions to the transporter. 2. Conformational change in the transporter protein, allowing GABA to move across the membrane. 3. Release of GABA and Na+ ions on the intracellular side of the membrane. 4. Return of the transporter to its initial conformation. GABA transporter activity is essential for maintaining proper neuronal function. Dysregulation of GABA transporter activity has been implicated in various neurological disorders, including epilepsy, anxiety disorders, and depression.'
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Protein | Definition | Taxonomy |
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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 |