Target type: biologicalprocess
The regulated release of gamma-aminobutyric acid by a cell or a tissue. The gamma-aminobutyric acid is the principal inhibitory neurotransmitter in the brain but is also found in several extraneural tissues. [GOC:ef]
Gamma-aminobutyric acid (GABA) secretion is a complex process that involves multiple steps, from synthesis and packaging of the neurotransmitter to its release into the synaptic cleft.
1. **Synthesis:** GABA is synthesized from glutamate by the enzyme glutamate decarboxylase (GAD). This reaction takes place in the cytoplasm of GABAergic neurons.
2. **Packaging:** Once synthesized, GABA is transported into synaptic vesicles via a vesicular GABA transporter (VGAT). These vesicles are specialized compartments within the presynaptic terminal.
3. **Vesicle Docking and Priming:** GABA-filled vesicles dock and prime at the presynaptic membrane, ready for release. This process involves proteins such as synaptotagmin, SNAP-25, and syntaxin.
4. **Calcium-Dependent Exocytosis:** The arrival of an action potential at the presynaptic terminal triggers the opening of voltage-gated calcium channels. The influx of calcium ions initiates the fusion of the docked vesicles with the presynaptic membrane.
5. **GABA Release:** The fusion of the vesicle with the membrane releases GABA into the synaptic cleft, the space between the presynaptic and postsynaptic neurons.
6. **Reuptake:** After release, GABA is rapidly removed from the synaptic cleft by GABA transporters (GATs) located on both the presynaptic and postsynaptic neurons. This process is crucial for terminating GABAergic signaling and preventing excessive GABAergic activity.
7. **GABAergic Signaling:** GABA binds to GABA receptors on the postsynaptic neuron, leading to the activation of various intracellular signaling pathways. These pathways can have inhibitory effects on the postsynaptic neuron, reducing its excitability.
In summary, GABA secretion is a tightly regulated process that involves multiple steps from synthesis to release and reuptake. This intricate process plays a critical role in the modulation of neuronal activity and is essential for proper brain function.'
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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) |
| Voltage-dependent L-type calcium channel subunit beta-4 | A voltage-dependent L-type calcium channel subunit beta-4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00305] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| tacrine | tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease. Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. | acridines; aromatic amine | EC 3.1.1.7 (acetylcholinesterase) inhibitor |
| nimodipine | nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm. Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure. | 2-methoxyethyl ester; C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; isopropyl ester | antihypertensive agent; calcium channel blocker; cardiovascular drug; vasodilator agent |
| 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 |
| 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 | |
| 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 | |
| 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 | |
| kn 62 | KN 62: inhibitor of Ca/calmodulin-dependent protein kinase II | piperazines | |
| ith 4012 | |||
| az 11645373 | AZ 11645373: InChIKey: VQEHBLGYANQWEA-UHFFFAOYSA-N | ||
| az10606120 | AZ10606120: a P2X7 receptor antagonist | ||
| 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 | |||
| 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 |