gamma-aminobutyric acid (GABA) B receptor, 1 (GABBR1, GPRC3A)
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Function
- receptor for GABA Ca+2 required for high affinity binding to GABA
- activity of this receptor mediated by Gi-proteins
- inhibit adenylyl cyclase activity
- stimulates phospholipase A2
- activates K+ channels
- inactivates voltage-dependent Ca+2-channels
- modulates inositol phospholipids hydrolysis
- fine-tuning of inhibitory synaptic transmission
- pre-synaptic GABA-B-R inhibit neurotransmitter release via down-regulating high-voltage activated Ca+2 channels
- postsynaptic GABA-B-R decrease neuronal excitability via activating a inwardly rectifying K+ (Kir) conductance associated with late inhibitory postsynaptic potentials
- hippocampal long-term potentiation
- slow wave sleep
- muscle relaxation
- antinociception
- activated by (-)-baclofen, blocked by phaclofen.
Structure
- serpentine receptor
- heterodimer of GABA-B-R1 & GABA-B-R2, neither of which is effective on its own;
- homodimeric assembly does not seem to occur
Expression
- expressed in brain > heart, small intestine, uterus, kidney, lung, trachea, colon, small intestine, stomach, bone marrow, thymus, mammary gland.
- isoform 1A: granular cells, molecular layer
- isoform 1B: Purkinje cells
- soform 1E: peripheral tissues
More general terms
References
- ↑ VanDongen AM, Codina J, Olate J, Mattera R, Joho R, Birnbaumer L, Brown AM. Newly identified brain potassium channels gated by the guanine nucleotide binding protein Go. Science. 1988 Dec 9;242(4884):1433-7. PMID: https://www.ncbi.nlm.nih.gov/pubmed/3144040
- ↑ Baumann PA, Wicki P, Stierlin C, Waldmeier PC. Investigations on GABAB receptor-mediated autoinhibition of GABA release. Naunyn Schmiedebergs Arch Pharmacol. 1990 Jan-Feb;341(1-2):88-93. PMID: https://www.ncbi.nlm.nih.gov/pubmed/2156176
- ↑ UniProt http://www.uniprot.org/uniprot/Q9UBS5.html