Target type: biologicalprocess
Any process that activates or increases the frequency, rate or extent of the regulated release of gamma-aminobutyric acid. [GOC:ef]
Positive regulation of gamma-aminobutyric acid (GABA) secretion is a complex biological process involving multiple cellular mechanisms. GABA, an inhibitory neurotransmitter, plays a crucial role in modulating neuronal activity and regulating brain function. This process begins with the synthesis of GABA from glutamate by the enzyme glutamic acid decarboxylase (GAD) within GABAergic neurons. Once synthesized, GABA is packaged into synaptic vesicles by vesicular GABA transporter (VGAT). These vesicles are then transported to the presynaptic terminal, where they await release.
The release of GABA is triggered by the arrival of an action potential at the presynaptic terminal. This depolarization opens voltage-gated calcium channels, allowing calcium ions to influx into the terminal. The rise in intracellular calcium concentration triggers a cascade of events, ultimately leading to the fusion of synaptic vesicles with the presynaptic membrane and the release of GABA into the synaptic cleft.
Several factors can positively regulate GABA secretion. One important factor is the activity of presynaptic receptors, such as metabotropic glutamate receptors (mGluRs), which can enhance GABA release by stimulating intracellular signaling pathways that promote vesicle fusion. The presence of specific proteins, such as synaptotagmin and complexin, also plays a key role in facilitating vesicle fusion and GABA release.
Furthermore, the activity of certain neurotransmitters, like acetylcholine and serotonin, can enhance GABA secretion by modulating presynaptic signaling pathways. Finally, environmental factors, such as stress and exposure to certain drugs, can also influence GABA release by affecting the activity of signaling pathways involved in this process.
In summary, positive regulation of GABA secretion is a multi-faceted process that involves the coordinated action of multiple cellular components, including enzymes, transporters, receptors, signaling molecules, and ion channels. This process is crucial for maintaining proper neuronal function and regulating brain activity.'
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Protein | Definition | Taxonomy |
---|---|---|
P2X purinoceptor 7 | A P2X purinoceptor 7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99572] | Homo sapiens (human) |
Neurotensin receptor type 1 | A neurotensin receptor type 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30989] | 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 |
---|---|---|---|
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 |
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 | |
oxatomide | oxatomide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one substituted by a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group at position 1. It is an anti-allergic drug. oxatomide: structure; an anti-allergic & an anti-asthmatic | benzimidazoles; diarylmethane; N-alkylpiperazine | anti-allergic agent; anti-inflammatory agent; geroprotector; H1-receptor antagonist; serotonergic antagonist |
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid | 5'-phosphopyridoxal-6-azobenzene-2,4-disulfonic acid : An arenesulfonic acid that is pyridoxal 5'-phosphate carrying an additional 2,4-disulfophenylazo substituent at position 6. pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid: a novel antagonist that selectively blocks P2 purinoceptor receptors; a useful tool to study co-transmission in tissues when ATP and coexisting neurotransmitters act in concert | arenesulfonic acid; azobenzenes; methylpyridines; monohydroxypyridine; organic phosphate; pyridinecarbaldehyde | purinergic receptor P2X antagonist |
suramin | suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties. | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
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 |
alpha,beta-methyleneadenosine 5'-triphosphate | alpha,beta-methyleneadenosine 5'-triphosphate: do not confuse with beta,gamma-methylene ATP; RN given refers to parent cpd | nucleoside triphosphate analogue | |
n-(4,4-diphenyl-3-butenyl)nipecotic acid | N-(4,4-diphenyl-3-butenyl)nipecotic acid: structure given in first source | diarylmethane | |
sr 48692 | SR 48692: structure in first source; a neurotensin receptor-1 antagonist | N-acyl-amino acid | |
nnc 711 | NNC 711: structure in first source | ||
sk&f 100330-a | SK&F 100330-A: structure given in first source | ||
sb 203580 | imidazoles; monofluorobenzenes; pyridines; sulfoxide | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent | |
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 | |
8-azidoadenosine 5'-triphosphate | |||
6-thioinosine-5'-triphosphate | organic molecule | ||
mrs2159 | MRS2159: an antagonist of both P2X1 and P2X7 receptors | ||
imd 0354 | N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide: a cardioprotective agent that inhibits IkappaB kinase beta (IKKbeta); structure in first source | benzamides | |
neurotensin | |||
sr 142948 | SR 142948: structurally similar to SR-48692 | N-acyl-amino acid | |
kn 62 | KN 62: inhibitor of Ca/calmodulin-dependent protein kinase II | piperazines | |
nipecotic acid, (s)-isomer | (S)-nipecotic acid : The (S)-enantiomer of nipecotic acid. | nipecotic acid | |
2-ethoxy-N-[1-(phenylmethyl)-4-piperidinyl]benzamide | piperidines | ||
az 11645373 | AZ 11645373: InChIKey: VQEHBLGYANQWEA-UHFFFAOYSA-N | ||
nnc 05-2090 | NNC 05-2090: structure given in first source | carbazoles | |
sr 48527 | SR 48527: SR 48527 is the S-enantiomer; SR-49711 is the R-enantiomer | ||
sr 142948a | SR 142948A: structure in first source | ||
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | |||
az10606120 | AZ10606120: a P2X7 receptor antagonist | ||
snap 5114 | |||
ce 224,535 | CE 224,535: structure in first source | ||
a-438079 | |||
af 353 | 5-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source | ||
gsk1482160 | |||
neurotensin | neurotensin, Tyr(11)-: RN given refers to parent cpd & (D)-isomer; RN for cpd without isomeric designation not avail 5/91 | peptide hormone | human metabolite; mitogen; neurotransmitter; vulnerary |
nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source | ||
a-839977 | A-839977: a selective P2X7 receptor antagonist, analgesic; structure in first source | ||
jnj-47965567 | JNJ-47965567: a P2X7 purinergic receptor antagonist; structure in first source | ||
mk-8742 | elbasvir : A complex organic heterotetracyclic compound that is a hepatitis C virus nonstructural protein 5A inhibitor used in combination with grazoprevir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults. elbasvir: inhibits NS5A protein of hepatitis C virus | carbamate ester; imidazoles; L-valine derivative; N-acylpyrrolidine; organic heterotetracyclic compound; ring assembly | antiviral drug; hepatitis C virus nonstructural protein 5A inhibitor; hepatoprotective agent |