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Gene Review

ADRB1  -  adrenoceptor beta 1

Homo sapiens

Synonyms: ADRB1R, B1AR, BETA1AR, Beta-1 adrenergic receptor, Beta-1 adrenoceptor, ...
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Disease relevance of ADRB1


Psychiatry related information on ADRB1


High impact information on ADRB1


Chemical compound and disease context of ADRB1


Biological context of ADRB1


Anatomical context of ADRB1


Associations of ADRB1 with chemical compounds

  • When 300 nmol/L CGP 20712A was present as the sole antagonist, only a marginal shift of the concentration-response curve for (-)-epinephrine was usually observed, indicating that beta 1AR were not mediating the effect of these low concentrations of (-)-epinephrine [25].
  • Accordingly, we used the proline-rich third intracellular loop of the beta1-AR either as a glutathione S-transferase fusion protein in biochemical "pull-down" assays or as bait in the yeast two-hybrid system to search for interacting proteins [28].
  • Several G-protein coupled receptors, such as the beta1-adrenergic receptor (beta1-AR), contain polyproline motifs within their intracellular domains [28].
  • Direct binding of the beta1 adrenergic receptor to the cyclic AMP-dependent guanine nucleotide exchange factor CNrasGEF leads to Ras activation [29].
  • This epitope could be identified as a polyanionic stretch present in the second extracellular loop of both the beta1-adrenoceptor and the M2 acetylcholine receptor [30].
  • Ethnic differences in sensitivity to atenolol remained significant (P=0.006) after adjustment for beta1-AR and alpha2C-AR genotypes [31].

Physical interactions of ADRB1


Regulatory relationships of ADRB1


Other interactions of ADRB1

  • The 2.4-kilobase cDNA for the human beta 1AR encodes a protein of 477 amino acid residues that is 69% homologous with the avian beta AR but only 54% homologous with the human beta 2AR [23].
  • We conclude that rapid agonist-induced desensitization of the beta 1AR involves phosphorylation of the receptor by both PKA and at least beta ARK1 in intact cells [27].
  • We found that the GNB3 T allele produces a significant risk for AD in individuals homozygous for the ADRB1 C allele, suggesting that the combined effect of both polymorphisms influences AD susceptibility [38].
  • SR 59119A, salbutamol, and isoproterenol (ADRB3, ADRB2, and nonselective ADRB agonists, respectively) induced a concentration-dependent relaxation of placental artery rings obtained from women with uncomplicated or preeclamptic pregnancies [39].
  • Identification of the endophilins (SH3p4/p8/p13) as novel binding partners for the beta1-adrenergic receptor [28].

Analytical, diagnostic and therapeutic context of ADRB1


  1. Association between obesity and a polymorphism in the beta(1)-adrenoceptor gene (Gly389Arg ADRB1) in Caucasian women. Dionne, I.J., Garant, M.J., Nolan, A.A., Pollin, T.I., Lewis, D.G., Shuldiner, A.R., Poehlman, E.T. Int. J. Obes. Relat. Metab. Disord. (2002) [Pubmed]
  2. Chronic stress promotes tumor growth and angiogenesis in a mouse model of ovarian carcinoma. Thaker, P.H., Han, L.Y., Kamat, A.A., Arevalo, J.M., Takahashi, R., Lu, C., Jennings, N.B., Armaiz-Pena, G., Bankson, J.A., Ravoori, M., Merritt, W.M., Lin, Y.G., Mangala, L.S., Kim, T.J., Coleman, R.L., Landen, C.N., Li, Y., Felix, E., Sanguino, A.M., Newman, R.A., Lloyd, M., Gershenson, D.M., Kundra, V., Lopez-Berestein, G., Lutgendorf, S.K., Cole, S.W., Sood, A.K. Nat. Med. (2006) [Pubmed]
  3. Polymorphisms in the angiotensinogen and angiotensin II type 1 receptor gene are related to change in left ventricular mass during antihypertensive treatment: results from the Swedish Irbesartan Left Ventricular Hypertrophy Investigation versus Atenolol (SILVHIA) trial. Kurland, L., Melhus, H., Karlsson, J., Kahan, T., Malmqvist, K., Ohman, P., Nyström, F., Hägg, A., Lind, L. J. Hypertens. (2002) [Pubmed]
  4. Beta1-adrenoceptor gene variations: a role in idiopathic dilated cardiomyopathy? Podlowski, S., Wenzel, K., Luther, H.P., Müller, J., Bramlage, P., Baumann, G., Felix, S.B., Speer, A., Hetzer, R., Köpke, K., Hoehe, M.R., Wallukat, G. J. Mol. Med. (2000) [Pubmed]
  5. Polymorphism of beta-adrenergic receptors and susceptibility to open-angle glaucoma. Inagaki, Y., Mashima, Y., Fuse, N., Funayama, T., Ohtake, Y., Yasuda, N., Murakami, A., Hotta, Y., Fukuchi, T., Tsubota, K. Mol. Vis. (2006) [Pubmed]
  6. A polymorphism of the beta1-adrenergic receptor is associated with low extraversion. Stein, M.B., Schork, N.J., Gelernter, J. Biol. Psychiatry (2004) [Pubmed]
  7. Randomized, double-blind, crossover, placebo-controlled comparison of propranolol and betaxolol in the treatment of neuroleptic-induced akathisia. Dumon, J.P., Catteau, J., Lanvin, F., Dupuis, B.A. The American journal of psychiatry. (1992) [Pubmed]
  8. Metoprolol for intermittent explosive disorder. Mattes, J.A. The American journal of psychiatry. (1985) [Pubmed]
  9. Disrupted beta 1-adrenoceptor-G protein coupling in the temporal cortex of patients with Alzheimer's disease. Cowburn, R.F., Vestling, M., Fowler, C.J., Ravid, R., Winblad, B., O'Neill, C. Neurosci. Lett. (1993) [Pubmed]
  10. Repeated electroconvulsive shock prevents increased neocortical beta 1-adrenoceptor binding after DSP-4 treatment in rats. Dooley, D.J., Heal, D.J., Goodwin, G.M. Eur. J. Pharmacol. (1987) [Pubmed]
  11. Molecular mimicry between the immunodominant ribosomal protein P0 of Trypanosoma cruzi and a functional epitope on the human beta 1-adrenergic receptor. Ferrari, I., Levin, M.J., Wallukat, G., Elies, R., Lebesgue, D., Chiale, P., Elizari, M., Rosenbaum, M., Hoebeke, J. J. Exp. Med. (1995) [Pubmed]
  12. Demonstration of an in vivo functional beta 3-adrenoceptor in man. Enocksson, S., Shimizu, M., Lönnqvist, F., Nordenström, J., Arner, P. J. Clin. Invest. (1995) [Pubmed]
  13. Reduced beta 1 receptor messenger RNA abundance in the failing human heart. Bristow, M.R., Minobe, W.A., Raynolds, M.V., Port, J.D., Rasmussen, R., Ray, P.E., Feldman, A.M. J. Clin. Invest. (1993) [Pubmed]
  14. Mapping of a functional autoimmune epitope on the beta 1-adrenergic receptor in patients with idiopathic dilated cardiomyopathy. Magnusson, Y., Marullo, S., Hoyer, S., Waagstein, F., Andersson, B., Vahlne, A., Guillet, J.G., Strosberg, A.D., Hjalmarson, A., Hoebeke, J. J. Clin. Invest. (1990) [Pubmed]
  15. Aldosterone synthase (CYP11B2) -344 C/T polymorphism is related to antihypertensive response: result from the Swedish Irbesartan Left Ventricular Hypertrophy Investigation versus Atenolol (SILVHIA) trial. Kurland, L., Melhus, H., Karlsson, J., Kahan, T., Malmqvist, K., Ohman, P., Nyström, F., Hägg, A., Lind, L. Am. J. Hypertens. (2002) [Pubmed]
  16. The effect of Escherichia coli endotoxin on the adrenergic control of lipolysis in the human adipocyte. Forse, R.A., Leibel, R., Gagner, M. J. Surg. Res. (1989) [Pubmed]
  17. Disodium cromoglycate does not prevent terbutaline-induced desensitization of beta 2-adrenoceptor-mediated cardiovascular in vivo functions in human volunteers. Schäfers, R.F., Piest, U., von Birgelen, C., Jakubetz, J., Daul, A.E., Philipp, T., Brodde, O.E. J. Cardiovasc. Pharmacol. (1999) [Pubmed]
  18. On the physiologic role of beta-2 adrenoceptors in the human heart: in vitro and in vivo studies. Motomura, S., Reinhard-Zerkowski, H., Daul, A., Brodde, O.E. Am. Heart J. (1990) [Pubmed]
  19. Selectivity of antagonist and partial agonist activity of celiprolol in normal subjects. Wheeldon, N.M., McDevitt, D.G., Lipworth, B.J. British journal of clinical pharmacology. (1992) [Pubmed]
  20. Variability within alpha- and beta-adrenoreceptor genes as a predictor of cardiovascular function at rest and in response to mental challenge. McCaffery, J.M., Pogue-Geile, M.F., Ferrell, R.E., Petro, N., Manuck, S.B. J. Hypertens. (2002) [Pubmed]
  21. Detailed physical analysis of a 1.5-megabase YAC contig containing the MXI1 and ADRA2A genes. Manca, A., Volpi, E.V., Laficara, F., Muresu, R., Gray, I.C., Spurr, N.K., Nobile, C. Genomics (1997) [Pubmed]
  22. Pharmacogenomics and drug response in cardiovascular disorders. Siest, G., Jeannesson, E., Berrahmoune, H., Maumus, S., Marteau, J.B., Mohr, S., Visvikis, S. Pharmacogenomics (2004) [Pubmed]
  23. Cloning of the cDNA for the human beta 1-adrenergic receptor. Frielle, T., Collins, S., Daniel, K.W., Caron, M.G., Lefkowitz, R.J., Kobilka, B.K. Proc. Natl. Acad. Sci. U.S.A. (1987) [Pubmed]
  24. Resistance of the human beta 1-adrenergic receptor to agonist-mediated down-regulation. Role of the C terminus in determining beta-subtype degradation. Liang, W., Austin, S., Hoang, Q., Fishman, P.H. J. Biol. Chem. (2003) [Pubmed]
  25. Coexistence of functioning beta 1- and beta 2-adrenoceptors in single myocytes from human ventricle. del Monte, F., Kaumann, A.J., Poole-Wilson, P.A., Wynne, D.G., Pepper, J., Harding, S.E. Circulation (1993) [Pubmed]
  26. Interaction with cystic fibrosis transmembrane conductance regulator-associated ligand (CAL) inhibits beta1-adrenergic receptor surface expression. He, J., Bellini, M., Xu, J., Castleberry, A.M., Hall, R.A. J. Biol. Chem. (2004) [Pubmed]
  27. Phosphorylation and desensitization of the human beta 1-adrenergic receptor. Involvement of G protein-coupled receptor kinases and cAMP-dependent protein kinase. Freedman, N.J., Liggett, S.B., Drachman, D.E., Pei, G., Caron, M.G., Lefkowitz, R.J. J. Biol. Chem. (1995) [Pubmed]
  28. Identification of the endophilins (SH3p4/p8/p13) as novel binding partners for the beta1-adrenergic receptor. Tang, Y., Hu, L.A., Miller, W.E., Ringstad, N., Hall, R.A., Pitcher, J.A., DeCamilli, P., Lefkowitz, R.J. Proc. Natl. Acad. Sci. U.S.A. (1999) [Pubmed]
  29. Direct binding of the beta1 adrenergic receptor to the cyclic AMP-dependent guanine nucleotide exchange factor CNrasGEF leads to Ras activation. Pak, Y., Pham, N., Rotin, D. Mol. Cell. Biol. (2002) [Pubmed]
  30. Structural and functional analysis of the B cell epitopes recognized by anti-receptor autoantibodies in patients with Chagas' disease. Elies, R., Ferrari, I., Wallukat, G., Lebesgue, D., Chiale, P., Elizari, M., Rosenbaum, M., Hoebeke, J., Levin, M.J. J. Immunol. (1996) [Pubmed]
  31. Beta-1-adrenoceptor genetic variants and ethnicity independently affect response to beta-blockade. Kurnik, D., Li, C., Sofowora, G.G., Friedman, E.A., Muszkat, M., Xie, H.G., Harris, P.A., Williams, S.M., Nair, U.B., Wood, A.J., Stein, C.M. Pharmacogenet. Genomics (2008) [Pubmed]
  32. GIPC interacts with the beta1-adrenergic receptor and regulates beta1-adrenergic receptor-mediated ERK activation. Hu, L.A., Chen, W., Martin, N.P., Whalen, E.J., Premont, R.T., Lefkowitz, R.J. J. Biol. Chem. (2003) [Pubmed]
  33. Iodinated analogs of trimetoquinol as highly potent and selective beta 2-adrenoceptor ligands. De Los Angeles, J.E., Nikulin, V.I., Shams, G., Konkar, A.A., Mehta, R., Feller, D.R., Miller, D.D. J. Med. Chem. (1996) [Pubmed]
  34. Studies of the Common DIO2 Thr92Ala Polymorphism and Metabolic Phenotypes in 7342 Danish White Subjects. Grarup, N., Andersen, M.K., Andreasen, C.H., Albrechtsen, A., Borch-Johnsen, K., J??rgensen, T., Auwerx, J., Schmitz, O., Hansen, T., Pedersen, O. J. Clin. Endocrinol. Metab. (2007) [Pubmed]
  35. The beta 1-adrenoceptor as antigen: functional aspects. Wallukat, G., Kayser, A., Wollenberger, A. Eur. Heart J. (1995) [Pubmed]
  36. A proline-rich region of the third intracellular loop imparts phenotypic beta 1-versus beta 2-adrenergic receptor coupling and sequestration. Green, S.A., Liggett, S.B. J. Biol. Chem. (1994) [Pubmed]
  37. G protein-coupled receptor kinase 5 regulates beta 1-adrenergic receptor association with PSD-95. Hu, L.A., Chen, W., Premont, R.T., Cong, M., Lefkowitz, R.J. J. Biol. Chem. (2002) [Pubmed]
  38. Polymorphism in genes involved in adrenergic signaling associated with Alzheimer's. Bullido, M.J., Ramos, M.C., Ruiz-Gómez, A., Tutor, A.S., Sastre, I., Frank, A., Coria, F., Gil, P., Mayor, F., Valdivieso, F. Neurobiol. Aging (2004) [Pubmed]
  39. Stimulation of the ADRB3 adrenergic receptor induces relaxation of human placental arteries: influence of preeclampsia. Rouget, C., Barthez, O., Goirand, F., Leroy, M.J., Breuiller-Fouché, M., Rakotoniaina, Z., Guérard, P., Morcillo, E.J., Advenier, C., Sagot, P., Cabrol, D., Dumas, M., Bardou, M. Biol. Reprod. (2006) [Pubmed]
  40. Chromosomal organization of adrenergic receptor genes. Yang-Feng, T.L., Xue, F.Y., Zhong, W.W., Cotecchia, S., Frielle, T., Caron, M.G., Lefkowitz, R.J., Francke, U. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
  41. Analysis of beta-adrenergic receptor mRNA levels in human ventricular biopsy specimens by quantitative polymerase chain reactions: progressive reduction of beta 1-adrenergic receptor mRNA in heart failure. Engelhardt, S., Böhm, M., Erdmann, E., Lohse, M.J. J. Am. Coll. Cardiol. (1996) [Pubmed]
  42. Changes in cardiac beta 1- and beta 2-adrenoceptor densities after human cardiac transplantation: relation to transplant coronary vasculopathy and pretransplantation disease. von der Leyen, H., Steinfath, M., Hecht, A., Schmitz, W., Scholz, H., Neumann, K., Haverich, A., Heublein, B. Am. Heart J. (1992) [Pubmed]
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