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Beta-1 adrenergic receptor

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Beta-1 adrenergic receptor
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factoids
The beta-1 adrenergic receptor (β1 adrenoceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the human gene encoding it. It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue.

Receptor

Actions

Actions of the β1 receptor include:{|class="wikitable"!colspan=3| Effect/Tissue
Muscular|Increase cardiac output|cardiac muscle
|Increase heart rate (chronotropic effect)
sinoatrial node (SA node) FITZPATRICK, DAVID AUTHOR3=AUGUSTINE, GEORGE PUBLISHER = SINAUER YEAR = 2004 CHAPTER = TABLE 20:2 ISBN = 978-0-87893-725-7 DOI =,
heart atrium>atrial contractility (inotropic effect)|cardiac muscle
cardiac muscle automaticity>automaticityheart ventricle>ventricular cardiac muscle
cardiac muscle automaticity>automaticity|atrioventricular node (AV node)
|Relaxation
JOURNAL = UROLOGY ISSUE = 1 DATE = JANUARY 2013 DOI = 10.1016/J.UROLOGY.2012.09.011,
Exocrine|Renin release|juxtaglomerular cells.
|stimulate viscous, amylase-filled secretions|salivary glandsBOOK, Rang, H. P., Pharmacology, Churchill Livingstone, Edinburgh, 2003, 978-0-443-07145-4, Page 163
|Other|Lipolysis|adipose tissue.
The receptor is also present in the cerebral cortex.

Agonists

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

(Beta blockers)β1-selective antagonists include:

Mechanism in cardiac myocytes

Gs exerts its effects via two pathways. Firstly, it directly opens L-type calcium channels (LTCC) in the plasma membrane. Secondly, it renders adenylate cyclase activated, resulting in an increase of cAMP, activating protein kinase A (PKA) which in turn phosphorylates several targets, such as phospholamban, LTCC, Troponin I (TnI), and potassium channels. Phospholamban phosphorylates deactivates its function which is normally inhibition of SERCA on the sarcoplasmic reticulum (SR) in cardiac myocytes. Due to this, more calcium enters the SR and is therefore available for the next contraction. LTCC phosphorylatation increases its open probability and therefore allows more calcium to enter the myocyte upon cell depolarisation. Both of these mechanisms increase the available calcium for contraction and therefore increase inotropy. Conversely, TnI phosphorylation results in its facilitated dissociation of calcium from troponin C (TnC) which fastens the muscle relaxation (positive lusitropy). Potassium channel phosphorylates increases its open probability which results in shorter refractory period (because the cell repolarises faster), also increasing lusitropy. Furthermore, in nodal cells such as in the SA node, cAMP directly binds to and opens the HCN channels, increasing their open probability, which increases chronotropy.BOOK, Medical physiology : a cellular and molecular approach, Boron, Walter F.,, Boulpaep, Emile L., 9781437717532, Updated second, Philadelphia, PA, 756281854, Boron, Walter F., Boulpaep, Emile L., 2012,

Gene

Specific polymorphisms in the ADRB1 gene have been shown to affect the resting heart rate and can be involved in heart failure.WEB, Entrez Gene: ADRB1 adrenergic, beta-1-, receptor,weblink

Interactions

Beta-1 adrenergic receptor has been shown to interact with DLG4JOURNAL, Hu LA, Tang Y, Miller WE, Cong M, Lau AG, Lefkowitz RJ, Hall RA, 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, Dec 2000, 10995758, 10.1074/jbc.M005938200, and GIPC1.JOURNAL, Hu LA, Chen W, Martin NP, Whalen EJ, Premont RT, Lefkowitz RJ, GIPC interacts with the beta1-adrenergic receptor and regulates beta1-adrenergic receptor-mediated ERK activation, The Journal of Biological Chemistry, 278, 28, 26295–301, Jul 2003, 12724327, 10.1074/jbc.M212352200, Interaction between testosterone and β-1 ARs have been shown in anxiolytic behaviors in the basolateral amygdala.JOURNAL, Mard-Soltani M, Kesmati M, Khajehpour L, Rasekh A, Shamshirgar-Zadeh A, Interaction between Anxiolytic Effects of Testosterone and β-1 Adrenoceptors of Basolateral Amygdala, International Journal of Pharmacology, April 2012, 10.3923/ijp.2012.344.354, 8, 5, 344–354,

See also

References

{{reflist}}

Further reading

  • JOURNAL, Frielle T, Kobilka B, Lefkowitz RJ, Caron MG, Human beta 1- and beta 2-adrenergic receptors: structurally and functionally related receptors derived from distinct genes, Trends in Neurosciences, 11, 7, 321–4, Jul 1988, 2465637, 10.1016/0166-2236(88)90095-1,
  • JOURNAL, Muszkat M, 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, Aug 2007, 17329986, 10.1038/sj.clpt.6100142,
  • JOURNAL, Yang-Feng TL, Xue FY, Zhong WW, Cotecchia S, Frielle T, Caron MG, Lefkowitz RJ, Francke U, Chromosomal organization of adrenergic receptor genes, Proceedings of the National Academy of Sciences of the United States of America, 87, 4, 1516–20, Feb 1990, 2154750, 53506, 10.1073/pnas.87.4.1516,
  • JOURNAL, Forse RA, Leibel R, Gagner M, 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, Jan 1989, 2536864, 10.1016/0022-4804(89)90180-7,
  • JOURNAL, Frielle T, Collins S, Daniel KW, Caron MG, Lefkowitz RJ, Kobilka BK, 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, Nov 1987, 2825170, 299447, 10.1073/pnas.84.22.7920,
  • JOURNAL, Stiles GL, Strasser RH, Lavin TN, Jones LR, Caron MG, Lefkowitz RJ, 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, Jul 1983, 6305985,
  • JOURNAL, Hoehe MR, Otterud B, Hsieh WT, Martinez MM, Stauffer D, Holik J, Berrettini WH, Byerley WF, Gershon ES, Lalouel JM, Genetic mapping of adrenergic receptor genes in humans, Journal of Molecular Medicine, 73, 6, 299–306, Jun 1995, 7583452, 10.1007/BF00231616,
  • JOURNAL, Elies R, Ferrari I, Wallukat G, Lebesgue D, Chiale P, Elizari M, Rosenbaum M, Hoebeke J, Levin MJ, 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, Nov 1996, 8892658,
  • JOURNAL, Oldenhof J, Vickery R, Anafi M, Oak J, Ray A, Schoots O, Pawson T, von Zastrow M, Van Tol HH, SH3 binding domains in the dopamine D4 receptor, Biochemistry, 37, 45, 15726–36, Nov 1998, 9843378, 10.1021/bi981634+,
  • JOURNAL, 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, The Journal of Biological Chemistry, 274, 18, 12670–4, Apr 1999, 10212248, 10.1074/jbc.274.18.12670,
  • JOURNAL, 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, Human Mutation, 14, 3, 271, Sep 1999, 10477438, 10.1002/(SICI)1098-1004(1999)14:33.0.CO;2-Q,
  • JOURNAL, Tang Y, Hu LA, Miller WE, Ringstad N, Hall RA, Pitcher JA, DeCamilli P, Lefkowitz RJ, 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, Oct 1999, 10535961, 22990, 10.1073/pnas.96.22.12559,
  • JOURNAL, Podlowski S, Wenzel K, Luther HP, Müller J, Bramlage P, Baumann G, Felix SB, Speer A, Hetzer R, Köpke K, Hoehe MR, Wallukat G, Beta1-adrenoceptor gene variations: a role in idiopathic dilated cardiomyopathy?, Journal of Molecular Medicine, 78, 2, 87–93, 2000, 10794544, 10.1007/s001090000080,
  • JOURNAL, Shiina T, Kawasaki A, Nagao T, Kurose H, 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, Sep 2000, 10862778, 10.1074/jbc.M909757199,
  • JOURNAL, Hu LA, Tang Y, Miller WE, Cong M, Lau AG, Lefkowitz RJ, Hall RA, 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, Dec 2000, 10995758, 10.1074/jbc.M005938200,
  • JOURNAL, Börjesson 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, European Heart Journal, 21, 22, 1853–8, Nov 2000, 11052857, 10.1053/euhj.1999.1994,
  • JOURNAL, Xu J, Paquet M, Lau AG, Wood JD, Ross CA, Hall RA, 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, Nov 2001, 11526121, 10.1074/jbc.M107480200,
  • JOURNAL, Hu LA, Chen W, Premont RT, Cong M, Lefkowitz RJ, G protein-coupled receptor kinase 5 regulates beta 1-adrenergic receptor association with PSD-95, The Journal of Biological Chemistry, 277, 2, 1607–13, Jan 2002, 11700307, 10.1074/jbc.M107297200,
  • JOURNAL, 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, American Journal of Human Genetics, 70, 4, 935–42, Apr 2002, 11854867, 379121, 10.1086/339621,

External links

  • {{UCSC gene info|ADRB1}}
  • WEB,weblink β1-adrenoceptor, IUPHAR Database of Receptors and Ion Channels, International Union of Basic and Clinical Pharmacology,
{{G protein-coupled receptors|g1}}

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