Target type: biologicalprocess
The uptake of gamma-aminobutyric acid (GABA, 4-aminobutyrate) by neurons or glial cells. This process leads to inactivation and recycling of neurotransmitters. [ISBN:0123668387]
Gamma-aminobutyric acid (GABA) reuptake is a crucial process in the termination of GABAergic neurotransmission. GABA, the primary inhibitory neurotransmitter in the central nervous system, acts on GABA receptors to dampen neuronal activity. After GABA release from presynaptic neurons, it must be efficiently cleared from the synaptic cleft to prevent prolonged inhibition. This clearance is primarily achieved through the reuptake of GABA back into presynaptic terminals by a specialized membrane transporter known as GABA transporter 1 (GAT-1). GAT-1 is a high-affinity sodium-dependent transporter that utilizes the energy of the sodium gradient to move GABA against its concentration gradient. The process of GABA reuptake involves several key steps: 1) GABA binds to GAT-1 at the extracellular site. 2) Sodium ions bind to the transporter. 3) The binding of GABA and sodium induces conformational changes in GAT-1, leading to the translocation of GABA across the membrane into the presynaptic terminal. 4) Once inside the presynaptic terminal, GABA is either repackaged into synaptic vesicles for subsequent release or broken down by the enzyme GABA transaminase (GABA-T). GABA reuptake is essential for maintaining the proper balance of neuronal activity and is a critical target for pharmacological interventions. Inhibition of GABA reuptake, by blocking the activity of GAT-1, can enhance GABAergic transmission and has therapeutic implications for disorders characterized by neuronal hyperexcitability, such as anxiety, epilepsy, and Parkinson's disease. '
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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 GABA transporter 3 | A sodium- and chloride-dependent GABA transporter 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48066] | Homo sapiens (human) |
Sodium- and chloride-dependent betaine transporter | A 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 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) |
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 GABA transporter 3 | A sodium- and chloride-dependent GABA transporter 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48066] | Homo sapiens (human) |
Sodium- and chloride-dependent betaine transporter | A 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 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) |
Compound | Definition | Classes | Roles |
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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 |
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 | |
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 |