Page last updated: 2024-10-24

positive regulation of gamma-aminobutyric acid secretion

Definition

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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Proteins (3)

ProteinDefinitionTaxonomy
P2X purinoceptor 7A P2X purinoceptor 7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99572]Homo sapiens (human)
Neurotensin receptor type 1A 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 1A sodium- and chloride-dependent GABA transporter 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P30531]Homo sapiens (human)

Compounds (44)

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
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
oxatomideoxatomide : 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 acid5'-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
suraminsuramin : 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
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
tiagabine hydrochloridetiagabine 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.hydrochlorideanticonvulsant;
GABA reuptake inhibitor
alpha,beta-methyleneadenosine 5'-triphosphatealpha,beta-methyleneadenosine 5'-triphosphate: do not confuse with beta,gamma-methylene ATP; RN given refers to parent cpdnucleoside triphosphate analogue
n-(4,4-diphenyl-3-butenyl)nipecotic acidN-(4,4-diphenyl-3-butenyl)nipecotic acid: structure given in first sourcediarylmethane
sr 48692SR 48692: structure in first source; a neurotensin receptor-1 antagonistN-acyl-amino acid
nnc 711NNC 711: structure in first source
sk&f 100330-aSK&F 100330-A: structure given in first source
sb 203580imidazoles;
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 966CI 966: GABA uptake blocker; RN from Toxlitdiarylmethane
hinokininhinokinin : 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-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
8-azidoadenosine 5'-triphosphate
6-thioinosine-5'-triphosphateorganic molecule
mrs2159MRS2159: an antagonist of both P2X1 and P2X7 receptors
imd 0354N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide: a cardioprotective agent that inhibits IkappaB kinase beta (IKKbeta); structure in first sourcebenzamides
neurotensin
sr 142948SR 142948: structurally similar to SR-48692N-acyl-amino acid
kn 62KN 62: inhibitor of Ca/calmodulin-dependent protein kinase IIpiperazines
nipecotic acid, (s)-isomer(S)-nipecotic acid : The (S)-enantiomer of nipecotic acid.nipecotic acid
2-ethoxy-N-[1-(phenylmethyl)-4-piperidinyl]benzamidepiperidines
az 11645373AZ 11645373: InChIKey: VQEHBLGYANQWEA-UHFFFAOYSA-N
nnc 05-2090NNC 05-2090: structure given in first sourcecarbazoles
sr 48527SR 48527: SR 48527 is the S-enantiomer; SR-49711 is the R-enantiomer
sr 142948aSR 142948A: structure in first source
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride
az10606120AZ10606120: a P2X7 receptor antagonist
snap 5114
ce 224,535CE 224,535: structure in first source
a-438079
af 3535-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source
gsk1482160
neurotensinneurotensin, Tyr(11)-: RN given refers to parent cpd & (D)-isomer; RN for cpd without isomeric designation not avail 5/91peptide hormonehuman metabolite;
mitogen;
neurotransmitter;
vulnerary
nitd 609NITD 609: an antimalarial and coccidiostat; structure in first source
a-839977A-839977: a selective P2X7 receptor antagonist, analgesic; structure in first source
jnj-47965567JNJ-47965567: a P2X7 purinergic receptor antagonist; structure in first source
mk-8742elbasvir : 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