Beta-1 adrenergic receptor

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Adrenoceptor beta 1
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols ADRB1 ; ADRB1R; B1AR; BETA1AR; RHR
External IDs OMIM109630 MGI87937 HomoloGene20171 IUPHAR: 28 ChEMBL: 213 GeneCards: ADRB1 Gene
RNA expression pattern
PBB GE ADRB1 208214 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 153 11554
Ensembl ENSG00000043591 ENSMUSG00000035283
UniProt P08588 P34971
RefSeq (mRNA) NM_000684 NM_007419
RefSeq (protein) NP_000675 NP_031445
Location (UCSC) Chr 10:
115.8 – 115.81 Mb
Chr 19:
56.72 – 56.72 Mb
PubMed search [1] [2]

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[edit]

Actions[edit]

Actions of the β1 receptor include:

Agonists[edit]

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:

Antagonists[edit]

(Beta blockers) β1-selective ones are:

Mechanism[edit]

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

Gene[edit]

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

Interactions[edit]

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[edit]

References[edit]

  1. ^ a b "Entrez Gene: ADRB1 adrenergic, beta-1-, receptor". 
  2. ^ a b c d e Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 163
  3. ^ a b c d e Fitzpatrick, David; Purves, Dale; Augustine, George (2004). "Table 20:2". Neuroscience (Third ed.). Sunderland, Mass: Sinauer. ISBN 0-87893-725-0. 
  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 et al. (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. doi:10.1074/jbc.M005938200. PMID 10995758. 
  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. doi:10.1074/jbc.M212352200. PMID 12724327. 
  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. doi:10.3923/ijp.2012.344.354. 

External links[edit]

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

Further reading[edit]

  • 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. doi:10.1016/0166-2236(88)90095-1. PMID 2465637. 
  • 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. doi:10.1038/sj.clpt.6100142. PMID 17329986. 
  • Yang-Feng TL, Xue FY, Zhong WW, Cotecchia S, Frielle T, Caron MG et al. (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. doi:10.1073/pnas.87.4.1516. PMC 53506. PMID 2154750. 
  • 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. doi:10.1016/0022-4804(89)90180-7. PMID 2536864. 
  • 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. doi:10.1073/pnas.84.22.7920. PMC 299447. PMID 2825170. 
  • 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. PMID 6305985. 
  • Hoehe MR, Otterud B, Hsieh WT, Martinez MM, Stauffer D, Holik J et al. (Jun 1995). "Genetic mapping of adrenergic receptor genes in humans". Journal of Molecular Medicine 73 (6): 299–306. doi:10.1007/BF00231616. PMID 7583452. 
  • Elies R, Ferrari I, Wallukat G, Lebesgue D, Chiale P, Elizari M et al. (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. PMID 8892658. 
  • Oldenhof J, Vickery R, Anafi M, Oak J, Ray A, Schoots O et al. (Nov 1998). "SH3 binding domains in the dopamine D4 receptor". Biochemistry 37 (45): 15726–36. doi:10.1021/bi981634. PMID 9843378. 
  • 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. doi:10.1074/jbc.274.18.12670. PMID 10212248. 
  • 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. doi:10.1002/(SICI)1098-1004(1999)14:3<271::AID-HUMU14>3.0.CO;2-Q. PMID 10477438. 
  • Tang Y, Hu LA, Miller WE, Ringstad N, Hall RA, Pitcher JA et al. (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. doi:10.1073/pnas.96.22.12559. PMC 22990. PMID 10535961. 
  • Podlowski S, Wenzel K, Luther HP, Müller J, Bramlage P, Baumann G et al. (2000). "Beta1-adrenoceptor gene variations: a role in idiopathic dilated cardiomyopathy?". Journal of Molecular Medicine 78 (2): 87–93. doi:10.1007/s001090000080. PMID 10794544. 
  • 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. doi:10.1074/jbc.M909757199. PMID 10862778. 
  • Hu LA, Tang Y, Miller WE, Cong M, Lau AG, Lefkowitz RJ et al. (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. doi:10.1074/jbc.M005938200. PMID 10995758. 
  • 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. doi:10.1053/euhj.1999.1994. PMID 11052857. 
  • 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. doi:10.1074/jbc.M107480200. PMID 11526121. 
  • 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. doi:10.1074/jbc.M107297200. PMID 11700307. 
  • Ranade K, Jorgenson E, Sheu WH, Pei D, Hsiung CA, Chiang FT et al. (Apr 2002). "A polymorphism in the beta1 adrenergic receptor is associated with resting heart rate". American Journal of Human Genetics 70 (4): 935–42. doi:10.1086/339621. PMC 379121. PMID 11854867.