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Beta-1 adrenergic receptor

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Title: Beta-1 adrenergic receptor  
Author: World Heritage Encyclopedia
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Subject: Norepinephrine, Discovery and development of beta-adrenergic receptor antagonists (beta-blockers), Iodocyanopindolol, Cyanopindolol, Beta-2 adrenergic receptor
Publisher: World Heritage Encyclopedia

Beta-1 adrenergic receptor

Adrenoceptor beta 1
Available structures
PDB Ortholog search: PDBe, RCSB
Symbols  ; ADRB1R; B1AR; BETA1AR; RHR
External IDs IUPHAR: ChEMBL: GeneCards:
RNA expression pattern
Species Human Mouse
RefSeq (mRNA)
RefSeq (protein)
Location (UCSC)
PubMed search

The beta-1 adrenergic receptor1 adrenoreceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the human gene encoding it.[1] It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue.


  • Receptor 1
    • Actions 1.1
    • Agonists 1.2
    • Antagonists 1.3
    • Mechanism 1.4
  • Gene 2
  • Interactions 3
  • See also 4
  • References 5
  • External links 6
  • Further reading 7



Actions of the β1 receptor include:


Isoprenaline has higher affinity for β1 than adrenaline, which, in turn, binds with higher affinity than noradrenaline at physiologic concentrations. Selective agonists to the beta-1 receptor are:


(Beta blockers) β1-selective ones are:


Gs renders adenylate cyclase activated, resulting in increase of cAMP.


Specific polymorphisms in the ADRB1 gene have been shown to affect the resting heart rate and can be involved in heart failure.[1]


Beta-1 adrenergic receptor has been shown to interact with DLG4[5] and GIPC1.[6] Interaction between testosterone and β-1 ARs have been shown in anxiolytic behaviors in the basolateral amygdala.[7]

See also


  1. ^ a b "Entrez Gene: ADRB1 adrenergic, beta-1-, receptor". 
  2. ^ a b c d e Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone.   Page 163
  3. ^ a b c d e Fitzpatrick, David; Purves, Dale; Augustine, George (2004). "Table 20:2". Neuroscience (Third ed.). Sunderland, Mass: Sinauer.  
  4. ^ American Society of Health-System Pharmacists, Inc. (2005-01-01). "Bisoprolol". MedlinePlus Drug Information. U.S. National Library of Medicine, National Institutes of Health. Archived from the original on 2008-05-20. Retrieved 2008-06-06. 
  5. ^ Hu LA, Tang Y, Miller WE, Cong M, Lau AG, Lefkowitz RJ, Hall RA (Dec 2000). "beta 1-adrenergic receptor association with PSD-95. Inhibition of receptor internalization and facilitation of beta 1-adrenergic receptor interaction with N-methyl-D-aspartate receptors". The Journal of Biological Chemistry 275 (49): 38659–66.  
  6. ^ Hu LA, Chen W, Martin NP, Whalen EJ, Premont RT, Lefkowitz RJ (Jul 2003). "GIPC interacts with the beta1-adrenergic receptor and regulates beta1-adrenergic receptor-mediated ERK activation". The Journal of Biological Chemistry 278 (28): 26295–301.  
  7. ^ Mard-Soltani M, Kesmati M, Khajehpour L, Rasekh A, Shamshirgar-Zadeh A (April 2012). "Interaction between Anxiolytic Effects of Testosterone and β-1 Adrenoceptors of Basolateral Amygdala". International Journal of Pharmacology 8 (5): 344–354.  

External links

  • -adrenoceptor"1"β. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading

  • Frielle T, Kobilka B, Lefkowitz RJ, Caron MG (Jul 1988). "Human beta 1- and beta 2-adrenergic receptors: structurally and functionally related receptors derived from distinct genes". Trends in Neurosciences 11 (7): 321–4.  
  • Muszkat M (Aug 2007). "Interethnic differences in drug response: the contribution of genetic variability in beta adrenergic receptor and cytochrome P4502C9". Clinical Pharmacology and Therapeutics 82 (2): 215–8.  
  • Yang-Feng TL, Xue FY, Zhong WW, Cotecchia S, Frielle T, Caron MG, Lefkowitz RJ, Francke U (Feb 1990). "Chromosomal organization of adrenergic receptor genes". Proceedings of the National Academy of Sciences of the United States of America 87 (4): 1516–20.  
  • Forse RA, Leibel R, Gagner M (Jan 1989). "The effect of Escherichia coli endotoxin on the adrenergic control of lipolysis in the human adipocyte". The Journal of Surgical Research 46 (1): 41–8.  
  • Frielle T, Collins S, Daniel KW, Caron MG, Lefkowitz RJ, Kobilka BK (Nov 1987). "Cloning of the cDNA for the human beta 1-adrenergic receptor". Proceedings of the National Academy of Sciences of the United States of America 84 (22): 7920–4.  
  • Stiles GL, Strasser RH, Lavin TN, Jones LR, Caron MG, Lefkowitz RJ (Jul 1983). "The cardiac beta-adrenergic receptor. Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by photoaffinity labeling". The Journal of Biological Chemistry 258 (13): 8443–9.  
  • Hoehe MR, Otterud B, Hsieh WT, Martinez MM, Stauffer D, Holik J, Berrettini WH, Byerley WF, Gershon ES, Lalouel JM (Jun 1995). "Genetic mapping of adrenergic receptor genes in humans". Journal of Molecular Medicine 73 (6): 299–306.  
  • Elies R, Ferrari I, Wallukat G, Lebesgue D, Chiale P, Elizari M, Rosenbaum M, Hoebeke J, Levin MJ (Nov 1996). "Structural and functional analysis of the B cell epitopes recognized by anti-receptor autoantibodies in patients with Chagas' disease". Journal of Immunology 157 (9): 4203–11.  
  • Oldenhof J, Vickery R, Anafi M, Oak J, Ray A, Schoots O, Pawson T, von Zastrow M, Van Tol HH (Nov 1998). "SH3 binding domains in the dopamine D4 receptor". Biochemistry 37 (45): 15726–36.  
  • Mason DA, Moore JD, Green SA, Liggett SB (Apr 1999). "A gain-of-function polymorphism in a G-protein coupling domain of the human beta1-adrenergic receptor". The Journal of Biological Chemistry 274 (18): 12670–4.  
  • Moore JD, Mason DA, Green SA, Hsu J, Liggett SB (Sep 1999). "Racial differences in the frequencies of cardiac beta(1)-adrenergic receptor polymorphisms: analysis of c145A>G and c1165G>C". Human Mutation 14 (3): 271.  
  • Tang Y, Hu LA, Miller WE, Ringstad N, Hall RA, Pitcher JA, DeCamilli P, Lefkowitz RJ (Oct 1999). "Identification of the endophilins (SH3p4/p8/p13) as novel binding partners for the beta1-adrenergic receptor". Proceedings of the National Academy of Sciences of the United States of America 96 (22): 12559–64.  
  • Podlowski S, Wenzel K, Luther HP, Müller J, Bramlage P, Baumann G, Felix SB, Speer A, Hetzer R, Köpke K, Hoehe MR, Wallukat G (2000). "Beta1-adrenoceptor gene variations: a role in idiopathic dilated cardiomyopathy?". Journal of Molecular Medicine 78 (2): 87–93.  
  • Shiina T, Kawasaki A, Nagao T, Kurose H (Sep 2000). "Interaction with beta-arrestin determines the difference in internalization behavor between beta1- and beta2-adrenergic receptors". The Journal of Biological Chemistry 275 (37): 29082–90.  
  • Hu LA, Tang Y, Miller WE, Cong M, Lau AG, Lefkowitz RJ, Hall RA (Dec 2000). "beta 1-adrenergic receptor association with PSD-95. Inhibition of receptor internalization and facilitation of beta 1-adrenergic receptor interaction with N-methyl-D-aspartate receptors". The Journal of Biological Chemistry 275 (49): 38659–66.  
  • Börjesson M, Magnusson Y, Hjalmarson A, Andersson B (Nov 2000). "A novel polymorphism in the gene coding for the beta(1)-adrenergic receptor associated with survival in patients with heart failure". European Heart Journal 21 (22): 1853–8.  
  • Xu J, Paquet M, Lau AG, Wood JD, Ross CA, Hall RA (Nov 2001). "beta 1-adrenergic receptor association with the synaptic scaffolding protein membrane-associated guanylate kinase inverted-2 (MAGI-2). Differential regulation of receptor internalization by MAGI-2 and PSD-95". The Journal of Biological Chemistry 276 (44): 41310–7.  
  • Hu LA, Chen W, Premont RT, Cong M, Lefkowitz RJ (Jan 2002). "G protein-coupled receptor kinase 5 regulates beta 1-adrenergic receptor association with PSD-95". The Journal of Biological Chemistry 277 (2): 1607–13.  
  • 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 (Apr 2002). "A polymorphism in the beta1 adrenergic receptor is associated with resting heart rate". American Journal of Human Genetics 70 (4): 935–42.  

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