Gamma-aminobutyric acid type B receptor subunit 1
Details
- Name
- Gamma-aminobutyric acid type B receptor subunit 1
- Synonyms
- GABA-B receptor 1
- GPRC3A
- Gene Name
- GABBR1
- Organism
- Humans
- Amino acid sequence
>lcl|BSEQ0000433|Gamma-aminobutyric acid type B receptor subunit 1 MLLLLLLAPLFLRPPGAGGAQTPNATSEGCQIIHPPWEGGIRYRGLTRDQVKAINFLPVD YEIEYVCRGEREVVGPKVRKCLANGSWTDMDTPSRCVRICSKSYLTLENGKVFLTGGDLP ALDGARVDFRCDPDFHLVGSSRSICSQGQWSTPKPHCQVNRTPHSERRAVYIGALFPMSG GWPGGQACQPAVEMALEDVNSRRDILPDYELKLIHHDSKCDPGQATKYLYELLYNDPIKI ILMPGCSSVSTLVAEAARMWNLIVLSYGSSSPALSNRQRFPTFFRTHPSATLHNPTRVKL FEKWGWKKIATIQQTTEVFTSTLDDLEERVKEAGIEITFRQSFFSDPAVPVKNLKRQDAR IIVGLFYETEARKVFCEVYKERLFGKKYVWFLIGWYADNWFKIYDPSINCTVDEMTEAVE GHITTEIVMLNPANTRSISNMTSQEFVEKLTKRLKRHPEETGGFQEAPLAYDAIWALALA LNKTSGGGGRSGVRLEDFNYNNQTITDQIYRAMNSSSFEGVSGHVVFDASGSRMAWTLIE QLQGGSYKKIGYYDSTKDDLSWSKTDKWIGGSPPADQTLVIKTFRFLSQKLFISVSVLSS LGIVLAVVCLSFNIYNSHVRYIQNSQPNLNNLTAVGCSLALAAVFPLGLDGYHIGRNQFP FVCQARLWLLGLGFSLGYGSMFTKIWWVHTVFTKKEEKKEWRKTLEPWKLYATVGLLVGM DVLTLAIWQIVDPLHRTIETFAKEEPKEDIDVSILPQLEHCSSRKMNTWLGIFYGYKGLL LLLGIFLAYETKSVSTEKINDHRAVGMAIYNVAVLCLITAPVTMILSSQQDAAFAFASLA IVFSSYITLVVLFVPKMRRLITRGEWQSEAQDTMKTGSSTNNNEEEKSRLLEKENRELEK IIAEKEERVSELRHQLQSRQQLRSRRHPPTPPEPSGGLPRGPPEPPDRLSCDGSRVHLLY K
- Number of residues
- 961
- Molecular Weight
- 108319.4
- Theoretical pI
- 8.3
- GO Classification
- FunctionsG-protein coupled GABA receptor activityProcessesadenylate cyclase-inhibiting G-protein coupled receptor signaling pathway / gamma-aminobutyric acid signaling pathway / negative regulation of adenylate cyclase activity / synaptic transmissionComponentscell junction / cytoplasm / dendrite / extracellular region / G-protein coupled receptor heterodimeric complex / integral component of plasma membrane / plasma membrane / postsynaptic membrane / presynaptic membrane
- General Function
- G-protein coupled gaba receptor activity
- Specific Function
- Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis. Calcium is required for high affinity binding to GABA. Plays a critical role in the fine-tuning of inhibitory synaptic transmission. Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials. Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception. Activated by (-)-baclofen, cgp27492 and blocked by phaclofen.Isoform 1E may regulate the formation of functional GABBR1/GABBR2 heterodimers by competing for GABBR2 binding. This could explain the observation that certain small molecule ligands exhibit differential affinity for central versus peripheral sites.
- Pfam Domain Function
- Transmembrane Regions
- 592-612 632-652 668-688 711-731 769-789 805-825 834-854
- Cellular Location
- Cell membrane
- Gene sequence
>lcl|BSEQ0010206|Gamma-aminobutyric acid type B receptor subunit 1 (GABBR1) ATGTTGCTGCTGCTGCTACTGGCGCCACTCTTCCTCCGCCCCCCGGGCGCGGGCGGGGCG CAGACCCCCAACGCCACCTCAGAAGGTTGCCAGATCATACACCCGCCCTGGGAAGGGGGC ATCAGGTACCGGGGCCTGACTCGGGACCAGGTGAAGGCTATCAACTTCCTGCCAGTGGAC TATGAGATTGAGTATGTGTGCCGGGGGGAGCGCGAGGTGGTGGGGCCCAAGGTCCGCAAG TGCCTGGCCAACGGCTCCTGGACAGATATGGACACACCCAGCCGCTGTGTCCGAATCTGC TCCAAGTCTTATTTGACCCTGGAAAATGGGAAGGTTTTCCTGACGGGTGGGGACCTCCCA GCTCTGGACGGAGCCCGGGTGGATTTCCGGTGTGACCCCGACTTCCATCTGGTGGGCAGC TCCCGGAGCATCTGTAGTCAGGGCCAGTGGAGCACCCCCAAGCCCCACTGCCAGGTGAAT CGAACGCCACACTCAGAACGGCGCGCAGTGTACATCGGGGCACTGTTTCCCATGAGCGGG GGCTGGCCAGGGGGCCAGGCCTGCCAGCCCGCGGTGGAGATGGCGCTGGAGGACGTGAAT AGCCGCAGGGACATCCTGCCGGACTATGAGCTCAAGCTCATCCACCACGACAGCAAGTGT GATCCAGGCCAAGCCACCAAGTACCTATATGAGCTGCTCTACAACGACCCTATCAAGATC ATCCTTATGCCTGGCTGCAGCTCTGTCTCCACGCTGGTGGCTGAGGCTGCTAGGATGTGG AACCTCATTGTGCTTTCCTATGGCTCCAGCTCACCAGCCCTGTCAAACCGGCAGCGTTTC CCCACTTTCTTCCGAACGCACCCATCAGCCACACTCCACAACCCTACCCGCGTGAAACTC TTTGAAAAGTGGGGCTGGAAGAAGATTGCTACCATCCAGCAGACCACTGAGGTCTTCACT TCGACTCTGGACGACCTGGAGGAACGAGTGAAGGAGGCTGGAATTGAGATTACTTTCCGC CAGAGTTTCTTCTCAGATCCAGCTGTGCCCGTCAAAAACCTGAAGCGCCAGGATGCCCGA ATCATCGTGGGACTTTTCTATGAGACTGAAGCCCGGAAAGTTTTTTGTGAGGTGTACAAG GAGCGTCTCTTTGGGAAGAAGTACGTCTGGTTCCTCATTGGGTGGTATGCTGACAATTGG TTCAAGATCTACGACCCTTCTATCAACTGCACAGTGGATGAGATGACTGAGGCGGTGGAG GGCCACATCACAACTGAGATTGTCATGCTGAATCCTGCCAATACCCGCAGCATTTCCAAC ATGACATCCCAGGAATTTGTGGAGAAACTAACCAAGCGACTGAAAAGACACCCTGAGGAG ACAGGAGGCTTCCAGGAGGCACCGCTGGCCTATGATGCCATCTGGGCCTTGGCACTGGCC CTGAACAAGACATCTGGAGGAGGCGGCCGTTCTGGTGTGCGCCTGGAGGACTTCAACTAC AACAACCAGACCATTACCGACCAAATCTACCGGGCAATGAACTCTTCGTCCTTTGAGGGT GTCTCTGGCCATGTGGTGTTTGATGCCAGCGGCTCTCGGATGGCATGGACGCTTATCGAG CAGCTTCAGGGTGGCAGCTACAAGAAGATTGGCTACTATGACAGCACCAAGGATGATCTT TCCTGGTCCAAAACAGATAAATGGATTGGAGGGTCCCCCCCAGCTGACCAGACCCTGGTC ATCAAGACATTCCGCTTCCTGTCACAGAAACTCTTTATCTCCGTCTCAGTTCTCTCCAGC CTGGGCATTGTCCTAGCTGTTGTCTGTCTGTCCTTTAACATCTACAACTCACATGTCCGT TATATCCAGAACTCACAGCCCAACCTGAACAACCTGACTGCTGTGGGCTGCTCACTGGCT TTAGCTGCTGTCTTCCCCCTGGGGCTCGATGGTTACCACATTGGGAGGAACCAGTTTCCT TTCGTCTGCCAGGCCCGCCTCTGGCTCCTGGGCCTGGGCTTTAGTCTGGGCTACGGTTCC ATGTTCACCAAGATTTGGTGGGTCCACACGGTCTTCACAAAGAAGGAAGAAAAGAAGGAG TGGAGGAAGACTCTGGAACCCTGGAAGCTGTATGCCACAGTGGGCCTGCTGGTGGGCATG GATGTCCTCACTCTCGCCATCTGGCAGATCGTGGACCCTCTGCACCGGACCATTGAGACA TTTGCCAAGGAGGAACCTAAGGAAGATATTGACGTCTCTATTCTGCCCCAGCTGGAGCAT TGCAGCTCCAGGAAGATGAATACATGGCTTGGCATTTTCTATGGTTACAAGGGGCTGCTG CTGCTGCTGGGAATCTTCCTTGCTTATGAGACCAAGAGTGTGTCCACTGAGAAGATCAAT GATCACCGGGCTGTGGGCATGGCTATCTACAATGTGGCAGTCCTGTGCCTCATCACTGCT CCTGTCACCATGATTCTGTCCAGCCAGCAGGATGCAGCCTTTGCCTTTGCCTCTCTTGCC ATAGTTTTCTCCTCCTATATCACTCTTGTTGTGCTCTTTGTGCCCAAGATGCGCAGGCTG ATCACCCGAGGGGAATGGCAGTCGGAGGCGCAGGACACCATGAAGACAGGGTCATCGACC AACAACAACGAGGAGGAGAAGTCCCGGCTGTTGGAGAAGGAGAACCGTGAACTGGAAAAG ATCATTGCTGAGAAAGAGGAGCGTGTCTCTGAACTGCGCCATCAACTCCAGTCTCGGCAG CAGCTCCGCTCCCGGCGCCACCCACCGACACCCCCAGAACCCTCTGGGGGCCTGCCCAGG GGACCCCCTGAGCCCCCCGACCGGCTTAGCTGTGATGGGAGTCGAGTGCATTTGCTTTAT AAGTGA
- Chromosome Location
- 6
- Locus
- 6p21.31
- External Identifiers
Resource Link UniProtKB ID Q9UBS5 UniProtKB Entry Name GABR1_HUMAN GenBank Protein ID 3892594 GenBank Gene ID AJ225028 GenAtlas ID GABBR1 HGNC ID HGNC:4070 - General References
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Drug Relations
- Drug Relations
DrugBank ID Name Drug group Pharmacological action? Actions Details DB00181 Baclofen approved unknown agonist Details DB00837 Progabide experimental yes agonist Details DB05010 SGS-742 investigational unknown Details DB06354 Tezampanel investigational unknown Details DB08891 Arbaclofen investigational yes agonist Details DB08892 Arbaclofen Placarbil investigational yes agonist Details DB02530 gamma-Aminobutyric acid approved, investigational unknown Details DB01956 Taurine approved, nutraceutical yes agonist Details DB00659 Acamprosate approved, investigational yes inhibitor Details DB12098 L-Baclofen investigational unknown agonist Details DB00363 Clozapine approved unknown positive modulator Details DB09072 Sodium oxybate approved unknown agonist Details