Beta-1 adrenergic receptor

Details

Name
Beta-1 adrenergic receptor
Synonyms
  • ADRB1R
  • B1AR
  • Beta-1 adrenoceptor
  • Beta-1 adrenoreceptor
Gene Name
ADRB1
Organism
Humans
Amino acid sequence
>lcl|BSEQ0010188|Beta-1 adrenergic receptor
MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV
WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC
TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM
AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP
LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV
FFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGP
PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV
Number of residues
477
Molecular Weight
51322.1
Theoretical pI
9.03
GO Classification
Functions
alpha-2A adrenergic receptor binding / beta-adrenergic receptor activity / beta1-adrenergic receptor activity / epinephrine binding / norepinephrine binding / PDZ domain binding / protein heterodimerization activity / Ras guanyl-nucleotide exchange factor activity / receptor signaling protein activity
Processes
activation of adenylate cyclase activity / adenylate cyclase-activating adrenergic receptor signaling pathway / brown fat cell differentiation / cell-cell signaling / diet induced thermogenesis / fear response / heat generation / intracellular signal transduction / negative regulation of multicellular organism growth / positive regulation of cAMP biosynthetic process / positive regulation of cAMP-mediated signaling / positive regulation of GTPase activity / positive regulation of heart rate by epinephrine-norepinephrine / positive regulation of the force of heart contraction by epinephrine-norepinephrine / response to cold / temperature homeostasis / vasodilation by norepinephrine-epinephrine involved in regulation of systemic arterial blood pressure
Components
early endosome / integral component of plasma membrane / plasma membrane
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Pfam Domain Function
Transmembrane Regions
56-84 94-120 133-154 173-196 223-248 320-349 355-377
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0010189|Beta-1 adrenergic receptor (ADRB1)
ATGGGCGCGGGGGTGCTCGTCCTGGGCGCCTCCGAGCCCGGTAACCTGTCGTCGGCCGCA
CCGCTCCCCGACGGCGCGGCCACCGCGGCGCGGCTGCTGGTGCCCGCGTCGCCGCCCGCC
TCGTTGCTGCCTCCCGCCAGCGAAAGCCCCGAGCCGCTGTCTCAGCAGTGGACAGCGGGC
ATGGGTCTGCTGATGGCGCTCATCGTGCTGCTCATCGTGGCGGGCAATGTGCTGGTGATC
GTGGCCATCGCCAAGACGCCGCGGCTGCAGACGCTCACCAACCTCTTCATCATGTCCCTG
GCCAGCGCCGACCTGGTCATGGGGCTGCTGGTGGTGCCGTTCGGGGCCACCATCGTGGTG
TGGGGCCGCTGGGAGTACGGCTCCTTCTTCTGCGAGCTGTGGACCTCAGTGGACGTGCTG
TGCGTGACGGCCAGCATCGAGACCCTGTGTGTCATTGCCCTGGACCGCTACCTCGCCATC
ACCTCGCCCTTCCGCTACCAGAGCCTGCTGACGCGCGCGCGGGCGCGGGGCCTCGTGTGC
ACCGTGTGGGCCATCTCGGCCCTGGTGTCCTTCCTGCCCATCCTCATGCACTGGTGGCGG
GCGGAGAGCGACGAGGCGCGCCGCTGCTACAACGACCCCAAGTGCTGCGACTTCGTCACC
AACCGGGCCTACGCCATCGCCTCGTCCGTAGTCTCCTTCTACGTGCCCCTGTGCATCATG
GCCTTCGTGTACCTGCGGGTGTTCCGCGAGGCCCAGAAGCAGGTGAAGAAGATCGACAGC
TGCGAGCGCCGTTTCCTCGGCGGCCCAGCGCGGCCGCCCTCGCCCTCGCCCTCGCCCGTC
CCCGCGCCCGCGCCGCCGCCCGGACCCCCGCGCCCCGCCGCCGCCGCCGCCACCGCCCCG
CTGGCCAACGGGCGTGCGGGTAAGCGGCGGCCCTCGCGCCTCGTGGCCCTGCGCGAGCAG
AAGGCGCTCAAGACGCTGGGCATCATCATGGGCGTCTTCACGCTCTGCTGGCTGCCCTTC
TTCCTGGCCAACGTGGTGAAGGCCTTCCACCGCGAGCTGGTGCCCGACCGCCTCTTCGTC
TTCTTCAACTGGCTGGGCTACGCCAACTCGGCCTTCAACCCCATCATCTACTGCCGCAGC
CCCGACTTCCGCAAGGCCTTCCAGGGACTGCTCTGCTGCGCGCGCAGGGCTGCCCGCCGG
CGCCACGCGACCCACGGAGACCGGCCGCGCGCCTCGGGCTGTCTGGCCCGGCCCGGACCC
CCGCCATCGCCCGGGGCCGCCTCGGACGACGACGACGACGATGTCGTCGGGGCCACGCCG
CCCGCGCGCCTGCTGGAGCCCTGGGCCGGCTGCAACGGCGGGGCGGCGGCGGACAGCGAC
TCGAGCCTGGACGAGCCGTGCCGCCCCGGCTTCGCCTCGGAATCCAAGGTGTAG
Chromosome Location
10
Locus
10q24-q26
External Identifiers
ResourceLink
UniProtKB IDP08588
UniProtKB Entry NameADRB1_HUMAN
GenBank Protein ID178200
GenBank Gene IDJ03019
GenAtlas IDADRB1
HGNC IDHGNC:285
General References
  1. Frielle T, Collins S, Daniel KW, Caron MG, Lefkowitz RJ, Kobilka BK: Cloning of the cDNA for the human beta 1-adrenergic receptor. Proc Natl Acad Sci U S A. 1987 Nov;84(22):7920-4. [PubMed:2825170]
  2. Moore JD, Mason DA, Green SA, Hsu J, Liggett SB: Racial differences in the frequencies of cardiac beta(1)-adrenergic receptor polymorphisms: analysis of c145A>G and c1165G>C. Hum Mutat. 1999 Sep 19;14(3):271. [PubMed:10477438]
  3. Deloukas P, Earthrowl ME, Grafham DV, Rubenfield M, French L, Steward CA, Sims SK, Jones MC, Searle S, Scott C, Howe K, Hunt SE, Andrews TD, Gilbert JG, Swarbreck D, Ashurst JL, Taylor A, Battles J, Bird CP, Ainscough R, Almeida JP, Ashwell RI, Ambrose KD, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Bates K, Beasley H, Bray-Allen S, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Cahill P, Camire D, Carter NP, Chapman JC, Clark SY, Clarke G, Clee CM, Clegg S, Corby N, Coulson A, Dhami P, Dutta I, Dunn M, Faulkner L, Frankish A, Frankland JA, Garner P, Garnett J, Gribble S, Griffiths C, Grocock R, Gustafson E, Hammond S, Harley JL, Hart E, Heath PD, Ho TP, Hopkins B, Horne J, Howden PJ, Huckle E, Hynds C, Johnson C, Johnson D, Kana A, Kay M, Kimberley AM, Kershaw JK, Kokkinaki M, Laird GK, Lawlor S, Lee HM, Leongamornlert DA, Laird G, Lloyd C, Lloyd DM, Loveland J, Lovell J, McLaren S, McLay KE, McMurray A, Mashreghi-Mohammadi M, Matthews L, Milne S, Nickerson T, Nguyen M, Overton-Larty E, Palmer SA, Pearce AV, Peck AI, Pelan S, Phillimore B, Porter K, Rice CM, Rogosin A, Ross MT, Sarafidou T, Sehra HK, Shownkeen R, Skuce CD, Smith M, Standring L, Sycamore N, Tester J, Thorpe A, Torcasso W, Tracey A, Tromans A, Tsolas J, Wall M, Walsh J, Wang H, Weinstock K, West AP, Willey DL, Whitehead SL, Wilming L, Wray PW, Young L, Chen Y, Lovering RC, Moschonas NK, Siebert R, Fechtel K, Bentley D, Durbin R, Hubbard T, Doucette-Stamm L, Beck S, Smith DR, Rogers J: The DNA sequence and comparative analysis of human chromosome 10. Nature. 2004 May 27;429(6990):375-81. [PubMed:15164054]
  4. Pak Y, Pham N, Rotin D: Direct binding of the beta1 adrenergic receptor to the cyclic AMP-dependent guanine nucleotide exchange factor CNrasGEF leads to Ras activation. Mol Cell Biol. 2002 Nov;22(22):7942-52. [PubMed:12391161]
  5. He J, Bellini M, Xu J, Castleberry AM, Hall RA: Interaction with cystic fibrosis transmembrane conductance regulator-associated ligand (CAL) inhibits beta1-adrenergic receptor surface expression. J Biol Chem. 2004 Nov 26;279(48):50190-6. Epub 2004 Sep 9. [PubMed:15358775]
  6. Cheng SB, Quinn JA, Graeber CT, Filardo EJ: Down-modulation of the G-protein-coupled estrogen receptor, GPER, from the cell surface occurs via a trans-Golgi-proteasome pathway. J Biol Chem. 2011 Jun 24;286(25):22441-55. doi: 10.1074/jbc.M111.224071. Epub 2011 May 2. [PubMed:21540189]
  7. Mason DA, Moore JD, Green SA, Liggett SB: A gain-of-function polymorphism in a G-protein coupling domain of the human beta1-adrenergic receptor. J Biol Chem. 1999 Apr 30;274(18):12670-4. [PubMed:10212248]
  8. Borjesson M, Magnusson Y, Hjalmarson A, Andersson B: A novel polymorphism in the gene coding for the beta(1)-adrenergic receptor associated with survival in patients with heart failure. Eur Heart J. 2000 Nov;21(22):1853-8. [PubMed:11052857]
  9. Ranade K, Jorgenson E, Sheu WH, Pei D, Hsiung CA, Chiang FT, Chen YD, Pratt R, Olshen RA, Curb D, Cox DR, Botstein D, Risch N: A polymorphism in the beta1 adrenergic receptor is associated with resting heart rate. Am J Hum Genet. 2002 Apr;70(4):935-42. Epub 2002 Feb 18. [PubMed:11854867]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00187EsmololapprovedyesantagonistDetails
DB00195Betaxololapproved, investigationalyesantagonistDetails
DB00221IsoetarineapprovedyesagonistDetails
DB00264Metoprololapproved, investigationalyesantagonistDetails
DB00335AtenololapprovedyesantagonistDetails
DB00373TimololapprovedyesantagonistDetails
DB00571Propranololapproved, investigationalyesantagonistDetails
DB00612BisoprololapprovedyesantagonistDetails
DB00841DobutamineapprovedyesagonistDetails
DB00866Alprenololexperimental, withdrawnyesantagonistDetails
DB00960Pindololapproved, investigationalyespartial agonistDetails
DB01064Isoprenalineapproved, investigationalyesagonistDetails
DB01102ArbutamineapprovedyesagonistDetails
DB01193Acebutololapproved, investigationalyespartial agonistDetails
DB01203NadololapprovedyesantagonistDetails
DB01210LevobunololapprovedyesantagonistDetails
DB01214MetipranololapprovedyesantagonistDetails
DB00521Carteololapprovedyespartial agonistDetails
DB00598LabetalolapprovedyesantagonistDetails
DB00668Epinephrineapproved, vet_approvedyesagonistDetails
DB01118Amiodaroneapproved, investigationalyesantagonistDetails
DB01136Carvedilolapproved, investigationalyesantagonistDetails
DB01151Desipramineapproved, investigationalunknownotherDetails
DB01295BevantololexperimentalyesantagonistDetails
DB01297PractololapprovedyesantagonistDetails
DB01580OxprenololapprovedyesantagonistDetails
DB01359Penbutololapproved, investigationalyesantagonistpartial agonistDetails
DB00368NorepinephrineapprovedyesagonistDetails
DB04855DronedaroneapprovedunknownDetails
DB04861Nebivololapproved, investigationalyesantagonistDetails
DB06262Droxidopaapproved, investigationalyesagonistDetails
DB01001Salbutamolapproved, vet_approvedunknownagonistDetails
DB00489SotalolapprovedyesantagonistDetails
DB01291PirbuterolapprovedunknownagonistDetails
DB01288Fenoterolapproved, investigationalunknownagonistDetails
DB00397Phenylpropanolamineapproved, vet_approved, withdrawnunknownagonistDetails
DB01407Clenbuterolapproved, investigational, vet_approvedunknownagonistDetails
DB083474-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrileexperimentalunknownDetails
DB085582-HYDROXYMETHYL-6-OCTYLSULFANYL-TETRAHYDRO-PYRAN-3,4,5-TRIOLexperimentalunknownDetails
DB08807Bopindololexperimentalyespartial agonistDetails
DB08808BupranololexperimentalyesantagonistDetails
DB00852Pseudoephedrineapprovedunknownagonistpartial agonistDetails
DB04846Celiprololapproved, investigationalyesantagonistDetails
DB01363Ephedra sinica rootnutraceuticalyesagonistDetails
DB06216AsenapineapprovedunknownantagonistDetails
DB00408LoxapineapprovedunknownbinderDetails
DB00248CabergolineapprovedunknownbinderDetails
DB09068Vortioxetineapproved, investigationalunknownligandDetails
DB09013BefunololexperimentalunknownDetails
DB00983Formoterolapproved, investigationalunknownagonistDetails
DB00938SalmeterolapprovedunknownagonistDetails
DB00871TerbutalineapprovedunknownantagonistDetails
DB01917PutrescineexperimentalunknownDetails
DB03566SpermidineexperimentalunknownDetails
DB00127Spermineexperimental, nutraceuticalunknownDetails
DB01182PropafenoneapprovedunknownantagonistDetails
DB09351Levobetaxololapproved, investigationalyesantagonistDetails
DB13781Xamoterolexperimentalyespartial agonistDetails
DB09204ArotinololinvestigationalyesantagonistDetails
DB00555Lamotrigineapproved, investigationalunknowninhibitorDetails
DB11124RacepinephrineapprovedyesagonistDetails
DB11278DL-MethylephedrineapprovedyesagonistDetails
DB00243Ranolazineapproved, investigationalnoantagonistDetails
DB00182Amphetamineapproved, illicit, investigationalunknownagonistDetails
DB00540NortriptylineapprovedunknownantagonistDetails
DB00726TrimipramineapprovedunknownbinderDetails
DB00334Olanzapineapproved, investigationalnoinhibitorDetails
DB00217BethanidineapprovedunknownantagonistDetails
DB01365MephentermineapprovedunknownagonistDetails
DB06726BufuralolexperimentalunknownantagonistDetails
DB13345Dihydroergocristineapproved, experimentalyesantagonistagonistDetails
DB01049Ergoloid mesylateapprovedyesantagonistagonistDetails
DB11273DihydroergocornineapprovedyesantagonistagonistDetails
DB11278DL-MethylephedrineapprovedyesagonistDetails