Beta-1 adrenergic receptor

The beta-1 adrenergic receptor (β₁ adrenoreceptor), also known as ADRB1, is an beta-adrenergic receptor, and also denotes the human gene encoding it.

Receptor

Actions

Actions of the β₁ receptor include:
*stimulate viscous, amylase-filled secretions from salivary glands cite book |author=Rang, H. P. |title=Pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2003 |pages= |isbn=0-443-07145-4 |oclc= |doi= Page 163 ]
* Increase cardiac output
** Increase heart rate cite book | author = Fitzpatrick, David; Purves, Dale; Augustine, George | title = Neuroscience | publisher = Sinauer | location = Sunderland, Mass | year = 2004 | | edition = Third Edition | chapter = Table 20:2 | pages = | isbn = 0-87893-725-0 | oclc = | doi = ] in sinoatrial node (SA node) (chronotropic effect)
** Increase atrial cardiac muscle contractility. (inotropic effect)
** Increases contractility and automaticity of ventricular cardiac muscle.
** Increases conduction and automaticity of atrioventricular node (AV node)

* Renin release from juxtaglomerular cells.
* Lipolysis in adipose tissue.
* Receptor also present in cerebral cortex.

Agonists

Isoprenaline has higher affinity for β₁ than noradrenaline, which, in turn, binds with higher affinity than adrenaline.
Selective agonists to the beta-1 receptor are:
*Denopamine
*Dobutamine (in cardiogenic shock)
*Xamoterol cite book |author=Rang, H. P. |title=Pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2003 |pages= |isbn=0-443-07145-4 |oclc= |doi= Page 163 ] (cardiac stimulant)

Antagonists

"(Beta blockers)"β1-selective ones are:
*Acebutolol (in hypertension, angina pectoris and arrhythmias)
*Atenolol (in hypertension, coronary heart disease, arrhythmias and myocardial infarction)
*Betaxolol (in hypertension and glaucoma)
*Bisoprololcite web | url = http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a693024.html | title = Bisoprolol | author = American Society of Health-System Pharmacists, Inc. | authorlink = | coauthors = | date = 2005-01-01 | format = | work = MedlinePlus Drug Information | publisher = U.S. National Library of Medicine, National Institutes of Health | pages = | language = | archiveurl = | archivedate = | quote = | accessdate = 2008-06-06] (in hypertension, coronary heart disease, arrhythmias, myocardial infarction and ischemic heart diseases)
*Esmolol (in arrhythmias)
*Metoprolol (in hypertension, coronary heart disease, myocardial infarction and heart failure)
*Nebivolol (in hypertension)

Mechanism

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

Gene

Specific polymorphisms in this gene have been shown to affect the resting heart rate and can be involved in heart failure.cite web | title = Entrez Gene: ADRB1 adrenergic, beta-1-, receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=153| accessdate = ]

ee also

*Other adrenergic receptors
**Alpha-1 adrenergic receptor
**Alpha-2 adrenergic receptor
**Beta-2 adrenergic receptor
**Beta-3 adrenergic receptor

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=Frielle T, Kobilka B, Lefkowitz RJ, Caron MG |title=Human beta 1- and beta 2-adrenergic receptors: structurally and functionally related receptors derived from distinct genes. |journal=Trends Neurosci. |volume=11 |issue= 7 |pages= 321–4 |year= 1989 |pmid= 2465637 |doi=
*cite journal | author=Muszkat M |title=Interethnic differences in drug response: the contribution of genetic variability in beta adrenergic receptor and cytochrome P4502C9. |journal=Clin. Pharmacol. Ther. |volume=82 |issue= 2 |pages= 215–8 |year= 2007 |pmid= 17329986 |doi= 10.1038/sj.clpt.6100142
*cite journal | author=Yang-Feng TL, Xue FY, Zhong WW, "et al." |title=Chromosomal organization of adrenergic receptor genes. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=87 |issue= 4 |pages= 1516–20 |year= 1990 |pmid= 2154750 |doi=
*cite journal | author=Forse RA, Leibel R, Gagner M |title=The effect of Escherichia coli endotoxin on the adrenergic control of lipolysis in the human adipocyte. |journal=J. Surg. Res. |volume=46 |issue= 1 |pages= 41–8 |year= 1989 |pmid= 2536864 |doi=
*cite journal | author=Frielle T, Collins S, Daniel KW, "et al." |title=Cloning of the cDNA for the human beta 1-adrenergic receptor. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=84 |issue= 22 |pages= 7920–4 |year= 1987 |pmid= 2825170 |doi=
*cite journal | author=Stiles GL, Strasser RH, Lavin TN, "et al." |title=The cardiac beta-adrenergic receptor. Structural similarities of beta 1 and beta 2 receptor subtypes demonstrated by photoaffinity labeling. |journal=J. Biol. Chem. |volume=258 |issue= 13 |pages= 8443–9 |year= 1983 |pmid= 6305985 |doi=
*cite journal | author=Hoehe MR, Otterud B, Hsieh WT, "et al." |title=Genetic mapping of adrenergic receptor genes in humans. |journal=J. Mol. Med. |volume=73 |issue= 6 |pages= 299–306 |year= 1995 |pmid= 7583452 |doi=
*cite journal | author=Elies R, Ferrari I, Wallukat G, "et al." |title=Structural and functional analysis of the B cell epitopes recognized by anti-receptor autoantibodies in patients with Chagas' disease. |journal=J. Immunol. |volume=157 |issue= 9 |pages= 4203–11 |year= 1996 |pmid= 8892658 |doi=
*cite journal | author=Oldenhof J, Vickery R, Anafi M, "et al." |title=SH3 binding domains in the dopamine D4 receptor. |journal=Biochemistry |volume=37 |issue= 45 |pages= 15726–36 |year= 1998 |pmid= 9843378 |doi= 10.1021/bi981634
*cite journal | author=Mason DA, Moore JD, Green SA, Liggett SB |title=A gain-of-function polymorphism in a G-protein coupling domain of the human beta1-adrenergic receptor. |journal=J. Biol. Chem. |volume=274 |issue= 18 |pages= 12670–4 |year= 1999 |pmid= 10212248 |doi=
*cite journal | author=Moore JD, Mason DA, Green SA, "et al." |title=Racial differences in the frequencies of cardiac beta(1)-adrenergic receptor polymorphisms: analysis of c145A>G and c1165G>C. |journal=Hum. Mutat. |volume=14 |issue= 3 |pages= 271 |year= 1999 |pmid= 10477438 |doi= 10.1002/(SICI)1098-1004(1999)14:3<271::AID-HUMU14>3.0.CO;2-Q |doilabel=10.1002/(SICI)1098-1004(1999)14:3271::AID-HUMU143.0.CO;2-Q
*cite journal | author=Tang Y, Hu LA, Miller WE, "et al." |title=Identification of the endophilins (SH3p4/p8/p13) as novel binding partners for the beta1-adrenergic receptor. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=96 |issue= 22 |pages= 12559–64 |year= 1999 |pmid= 10535961 |doi=
*cite journal | author=Podlowski S, Wenzel K, Luther HP, "et al." |title=Beta1-adrenoceptor gene variations: a role in idiopathic dilated cardiomyopathy? |journal=J. Mol. Med. |volume=78 |issue= 2 |pages= 87–93 |year= 2000 |pmid= 10794544 |doi=
*cite journal | author=Shiina T, Kawasaki A, Nagao T, Kurose H |title=Interaction with beta-arrestin determines the difference in internalization behavor between beta1- and beta2-adrenergic receptors. |journal=J. Biol. Chem. |volume=275 |issue= 37 |pages= 29082–90 |year= 2000 |pmid= 10862778 |doi= 10.1074/jbc.M909757199
*cite journal | author=Hu LA, Tang Y, Miller WE, "et al." |title=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. |journal=J. Biol. Chem. |volume=275 |issue= 49 |pages= 38659–66 |year= 2001 |pmid= 10995758 |doi= 10.1074/jbc.M005938200
*cite journal | author=Börjesson M, Magnusson Y, Hjalmarson A, Andersson B |title=A novel polymorphism in the gene coding for the beta(1)-adrenergic receptor associated with survival in patients with heart failure. |journal=Eur. Heart J. |volume=21 |issue= 22 |pages= 1853–8 |year= 2001 |pmid= 11052857 |doi= 10.1053/euhj.1999.1994
*cite journal | author=Xu J, Paquet M, Lau AG, "et al." |title=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. |journal=J. Biol. Chem. |volume=276 |issue= 44 |pages= 41310–7 |year= 2001 |pmid= 11526121 |doi= 10.1074/jbc.M107480200
*cite journal | author=Hu LA, Chen W, Premont RT, "et al." |title=G protein-coupled receptor kinase 5 regulates beta 1-adrenergic receptor association with PSD-95. |journal=J. Biol. Chem. |volume=277 |issue= 2 |pages= 1607–13 |year= 2002 |pmid= 11700307 |doi= 10.1074/jbc.M107297200
*cite journal | author=Ranade K, Jorgenson E, Sheu WH, "et al." |title=A polymorphism in the beta1 adrenergic receptor is associated with resting heart rate. |journal=Am. J. Hum. Genet. |volume=70 |issue= 4 |pages= 935–42 |year= 2002 |pmid= 11854867 |doi=

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