G protein-coupled GABA receptor activity
Definition
Target type: molecularfunction
Combining with the amino acid gamma-aminobutyric acid (GABA, 4-aminobutyrate) and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:ai, GOC:bf, IUPHAR_RECEPTOR:1276, Wikipedia:GABAB_receptor]
G protein-coupled GABA receptors (GABAu003csubu003eBu003c/subu003eRs) are members of the G protein-coupled receptor (GPCR) superfamily, which are integral membrane proteins that transduce extracellular signals into intracellular responses. GABAu003csubu003eBu003c/subu003eRs are unique among GPCRs in that they are heterodimers composed of two subunits, GABAu003csubu003eBu003c/subu003eR1 and GABAu003csubu003eBu003c/subu003eR2, which are required for receptor function. The GABAu003csubu003eBu003c/subu003eR1 subunit is responsible for binding GABA, while the GABAu003csubu003eBu003c/subu003eR2 subunit interacts with G proteins. Upon GABA binding, GABAu003csubu003eBu003c/subu003eRs activate Gu003csubu003ei/ou003c/subu003e proteins, which inhibit adenylyl cyclase activity, leading to a decrease in cAMP levels. In addition, Gu003csubu003ei/ou003c/subu003e proteins activate inwardly rectifying potassium (Ku003csupu003e+u003c/supu003e) channels, resulting in hyperpolarization of the membrane. This hyperpolarization can inhibit neuronal firing, contributing to the inhibitory effects of GABA. GABAu003csubu003eBu003c/subu003eRs are also known to activate phospholipase C (PLC) through Gu003csubu003equ003c/subu003e proteins, leading to the generation of inositol trisphosphate (IPu003csubu003e3u003c/subu003e) and diacylglycerol (DAG). IPu003csubu003e3u003c/subu003e mobilizes intracellular calcium stores, while DAG activates protein kinase C (PKC). The downstream signaling pathways activated by GABAu003csubu003eBu003c/subu003eRs are diverse and contribute to a wide range of physiological functions, including synaptic plasticity, neuroprotection, and modulation of pain perception.'
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Proteins (3)
| Protein | Definition | Taxonomy |
|---|---|---|
| Gamma-aminobutyric acid type B receptor subunit 1 | A gamma-aminobutyric acid type B receptor subunit 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UBS5] | Homo sapiens (human) |
| Gamma-aminobutyric acid type B receptor subunit 1 | A gamma-aminobutyric acid type B receptor subunit 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UBS5] | Homo sapiens (human) |
| Gamma-aminobutyric acid type B receptor subunit 2 | A gamma-aminobutyric acid type B receptor subunit 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O75899] | Homo sapiens (human) |
Compounds (13)
| 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 |
| baclofen | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant | |
| (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid | (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid: a GABA-C receptor antagonist; structure in first source | ||
| vigabatrin | gamma-amino acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor | |
| 4-amino-3-phenylbutyric acid | 4-amino-3-phenylbutyric acid: phenyl deriv of GABA; RN given refers to cpd without isomeric designation; structure | organonitrogen compound; organooxygen compound | |
| Arbaclofen | organonitrogen compound; organooxygen compound | ||
| 4-amino-3-(5-chloro-2-thienyl)butyric acid | 4-amino-3-(5-chloro-2-thienyl)butyric acid: binds GABA receptors; RN & structure given in first source | ||
| alpha-ethyl, alpha-methyl-thiobutyrolactone | tetrahydrothiophenes | ||
| cgp 36742 | (3-aminopropyl)(n-butyl)phosphinic acid: interacts preferably with GABA-B RECEPTORS (IC50=38 μM) and GABA-C receptors (IC50=62 μM) over GABA-A RECEPTORS (IC50=508 μM) | ||
| alpha-isopropyl-alpha-methyl-gamma-butyrolactone | alpha-isopropyl-alpha-methyl-gamma-butyrolactone: structure given in first source; picrotoxin receptor antagonist | ||
| (r,s)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3h-benzofuran-2-one | (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one: a positive allosteric modulator of GABAB receptors; structure in first source | ||
| cgp 7930 | 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol: structure in first source | alkylbenzene | |
| n,n'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine | N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine: structure in first source | aryl sulfide |