Beta-1 Adrenergic Receptor

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Beta-1 adrenergic receptor

The beta-1 adrenergic receptor (1 adrenoreceptor),also known as ADRB1, is a beta-adrenergic receptor,and also denotes the human gene encoding it.[1] It isa G-protein coupled receptor associated with the Gsheterotrimeric G-proteinand is expressed predominantlyin cardiac tissue.

1 Receptor

1.1 Actions

Actions of the 1receptor include:

stimulate viscous, amylase-filled secretions fromsalivary glands[2]

Increasecardiac output

Increase heart rate[3] in sinoatrial node (SAnode) (chronotropiceffect)

Increase atrial cardiac muscle contractility.(inotropiceffect)

Increases contractility and automaticity[3] ofventricularcardiac muscle.

Increases conduction and automaticity[3] ofatrioventricular node(AV node)

Reninrelease fromjuxtaglomerular cells.[3]

Lipolysisinadipose tissue.[3]

Receptor also present incerebral cortex.

1.2 Agonists

Isoprenaline has higher affinity for 1 than adrenaline,which, in turn, binds with higher affinity thannoradrenaline at physiologic concentrations. Selectiveagoniststo the beta-1 receptor are:

Denopamine

Dobutamine[2] (incardiogenic shock)

Xamoterol[2] (cardiac stimulant)

1.3 Antagonists

(Beta blockers)1-selective ones are:

Acebutolol (in hypertension, angina pectoris andarrhythmias)

Atenolol[2] (inhypertension,coronary heart disease,arrhythmiasandmyocardial infarction)

Betaxolol(inhypertensionandglaucoma)

Bisoprolol[4] (in hypertension, coronary heartdisease, arrhythmias, myocardial infarction andischemic heart diseases)

Esmolol(inarrhythmias)

Metoprolol[2] (inhypertension,coronary heart dis-ease,myocardial infarctionandheart failure)

Nebivolol(inhypertension)

Vortioxetine(antidepressant)

1.4 Mechanism

G renders adenylate cyclase activated, resulting in in-crease ofcAMP.

2 Gene

Specific polymorphisms in the ADRB1 gene have beenshown to affect the restingheart rateand can be involvedinheart failure.[1]

3 Interactions

Beta-1 adrenergic receptor has been shown to interactwithDLG4[5] andGIPC1.[6] Interaction between testos-terone and 1 ARs have been shown in anxiolytic be-haviors in the basolateral amygdala.[7]

4 See also

Otheradrenergic receptors

Alpha-1 adrenergic receptor

1
https://en.wikipedia.org/wiki/Alpha-1_adrenergic_receptorhttps://en.wikipedia.org/wiki/Adrenergic_receptorshttps://en.wikipedia.org/wiki/GIPC1https://en.wikipedia.org/wiki/DLG4https://en.wikipedia.org/wiki/Protein-protein_interactionhttps://en.wikipedia.org/wiki/Heart_failurehttps://en.wikipedia.org/wiki/Heart_ratehttps://en.wikipedia.org/wiki/Cyclic_adenosine_monophosphatehttps://en.wikipedia.org/wiki/Adenylate_cyclasehttps://en.wikipedia.org/wiki/Gs_alpha_subunithttps://en.wikipedia.org/wiki/Antidepressanthttps://en.wikipedia.org/wiki/Vortioxetinehttps://en.wikipedia.org/wiki/Hypertensionhttps://en.wikipedia.org/wiki/Nebivololhttps://en.wikipedia.org/wiki/Heart_failurehttps://en.wikipedia.org/wiki/Myocardial_infarctionhttps://en.wikipedia.org/wiki/Coronary_heart_diseasehttps://en.wikipedia.org/wiki/Coronary_heart_diseasehttps://en.wikipedia.org/wiki/Hypertensionhttps://en.wikipedia.org/wiki/Metoprololhttps://en.wikipedia.org/wiki/Arrhythmiahttps://en.wikipedia.org/wiki/Esmololhttps://en.wikipedia.org/wiki/Ischemic_heart_diseasehttps://en.wikipedia.org/wiki/Myocardial_infarctionhttps://en.wikipedia.org/wiki/Arrhythmiahttps://en.wikipedia.org/wiki/Coronary_heart_diseasehttps://en.wikipedia.org/wiki/Coronary_heart_diseasehttps://en.wikipedia.org/wiki/Hypertensionhttps://en.wikipedia.org/wiki/Bisoprololhttps://en.wikipedia.org/wiki/Glaucomahttps://en.wikipedia.org/wiki/Hypertensionhttps://en.wikipedia.org/wiki/Betaxololhttps://en.wikipedia.org/wiki/Myocardial_infarctionhttps://en.wikipedia.org/wiki/Arrhythmiahttps://en.wikipedia.org/wiki/Coronary_heart_diseasehttps://en.wikipedia.org/wiki/Hypertensionhttps://en.wikipedia.org/wiki/Atenololhttps://en.wikipedia.org/wiki/Arrhythmiahttps://en.wikipedia.org/wiki/Angina_pectorishttps://en.wikipedia.org/wiki/Hypertensionhttps://en.wikipedia.org/wiki/Acebutololhttps://en.wikipedia.org/wiki/Beta_blockerhttps://en.wikipedia.org/wiki/Cardiac_stimulanthttps://en.wikipedia.org/wiki/Xamoterolhttps://en.wikipedia.org/wiki/Cardiogenic_shockhttps://en.wikipedia.org/wiki/Dobutaminehttps://en.wikipedia.org/wiki/Denopaminehttps://en.wikipedia.org/wiki/Selective_agonisthttps://en.wikipedia.org/wiki/Selective_agonisthttps://en.wikipedia.org/wiki/Noradrenalinehttps://en.wikipedia.org/wiki/Adrenalinehttps://en.wikipedia.org/wiki/Isoprenalinehttps://en.wikipedia.org/wiki/Cerebral_cortexhttps://en.wikipedia.org/wiki/Adipose_tissuehttps://en.wikipedia.org/wiki/Lipolysishttps://en.wikipedia.org/wiki/Juxtaglomerular_cellshttps://en.wikipedia.org/wiki/Reninhttps://en.wikipedia.org/wiki/Atrioventricular_nodehttps://en.wikipedia.org/wiki/Cardiac_muscle_automaticityhttps://en.wikipedia.org/wiki/Heart_ventriclehttps://en.wikipedia.org/wiki/Cardiac_muscle_automaticityhttps://en.wikipedia.org/wiki/Inotropichttps://en.wikipedia.org/wiki/Cardiac_musclehttps://en.wikipedia.org/wiki/Heart_atriumhttps://en.wikipedia.org/wiki/Chronotropichttps://en.wikipedia.org/wiki/Sinoatrial_nodehttps://en.wikipedia.org/wiki/Heart_ratehttps://en.wikipedia.org/wiki/Cardiac_outputhttps://en.wikipedia.org/wiki/Salivary_glandhttps://en.wikipedia.org/wiki/Amylasehttps://en.wikipedia.org/wiki/Heterotrimeric_G-proteinhttps://en.wikipedia.org/wiki/Gs_alpha_subunithttps://en.wikipedia.org/wiki/G-protein_coupled_receptorhttps://en.wikipedia.org/wiki/Genehttps://en.wikipedia.org/wiki/Beta-adrenergic_receptor


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2 7 FURTHER READING

Alpha-2 adrenergic receptor



5 References

[1] Entrez Gene: ADRB1 adrenergic, beta-1-, receptor.

[2] Rang, H.P. (2003). Pharmacology. Edinburgh: ChurchillLivingstone. ISBN 0-443-07145-4. Page 163

[3] Fitzpatrick, David; Purves, Dale; Augustine, George(2004). Table 20:2. Neuroscience (Third ed.). Sunder-land, Mass: Sinauer.ISBN 0-87893-725-0.

[4] American Society of Health-System Pharmacists, Inc.(2005-01-01). Bisoprolol. MedlinePlus Drug Informa-tion

. U.S. National Library of Medicine, National Insti-tutes of Health. Archived fromthe originalon 2008-05-20. Retrieved 2008-06-06.

[5] Hu LA, Tang Y, Miller WE, Cong M, Lau AG, LefkowitzRJ, Hall RA (2000). beta 1-adrenergic receptor associ-ation with PSD-95. Inhibition of receptor internalizationand facilitation of beta 1-adrenergic receptor interactionwith N-methyl-D-aspartate receptors. J. Biol. Chem.275 (49): 3865966. doi:10.1074/jbc.M005938200.

PMID 10995758.

[6] Hu LA, Chen W, Martin NP, Whalen EJ, PremontRT, Lefkowitz RJ (2003). GIPC interacts with the

beta1-adrenergic receptor and regulates beta1-adrenergicreceptor-mediated ERK activation. J. Biol. Chem. 278(28): 26295301.doi:10.1074/jbc.M212352200.PMID12724327.

[7] Mard-Soltani M, Kesmati M, Khajehpour L, RasekhA, Shamshirgar-Zadeh A (April 2012). Interac-tion between Anxiolytic Effects of Testosterone and1 Adrenoceptors of Basolateral Amygdala. In-ternational Journal of Pharmacology 8 (5): 344354.doi:10.3923/ijp.2012.344.354.

6 External links "1-adrenoceptor. IUPHAR Database of Receptors

and Ion Channels. International Union of Basic andClinical Pharmacology.

7 Further reading

Frielle T, Kobilka B, Lefkowitz RJ, Caron MG(1989). Human beta 1- and beta 2-adrenergic re-ceptors: structurally and functionally related recep-

tors derived from distinct genes.. Trends Neurosci.11(7): 3214. doi:10.1016/0166-2236(88)90095-1.PMID 2465637.

Muszkat M (2007). Interethnic differences indrug response: the contribution of genetic vari-ability in beta adrenergic receptor and cytochromeP4502C9..Clin. Pharmacol. Ther. 82 (2): 2158.doi:10.1038/sj.clpt.6100142 .PMID 17329986.

Yang-Feng TL, Xue FY, Zhong WW, et al. (1990).Chromosomal organization of adrenergic receptorgenes.. Proc. Natl. Acad. Sci. U.S.A. 87 (4):15161520. doi:10.1073/pnas.87.4.1516. PMC53506.PMID 2154750.

Forse RA, Leibel R, Gagner M (1989). The ef-fect of Escherichia coli endotoxin on the adrener-gic control of lipolysis in the human adipocyte..J. Surg. Res. 46 (1): 418. doi:10.1016/0022-4804(89)90180-7.PMID 2536864.

Frielle T, Collins S, Daniel KW, et al.

(1987). Cloning of the cDNA for the hu-man beta 1-adrenergic receptor.. Proc. Natl.Acad. Sci. U.S.A. 84 (22): 79207924.doi:10.1073/pnas.84.22.7920. PMC 299447.PMID 2825170.

Stiles GL, Strasser RH, Lavin TN, et al. (1983).The cardiac beta-adrenergic receptor. Structuralsimilarities of beta 1 and beta 2 receptor subtypesdemonstrated by photoaffinity labeling.. J. Biol.Chem. 258 (13): 84438449.PMID 6305985.

Hoehe MR, Otterud B, Hsieh WT, et al. (1995).

Genetic mapping of adrenergic receptor genes inhumans.. J. Mol. Med. 73 (6): 299306.doi:10.1007/BF00231616.PMID 7583452.

Elies R, Ferrari I, Wallukat G, et al. (1996). Struc-tural and functional analysis of the B cell epitopesrecognized by anti-receptor autoantibodies in pa-tients with Chagas disease.. J. Immunol. 157(9):42034211.PMID 8892658.

Oldenhof J, Vickery R, Anafi M, et al. (1998).SH3 binding domains in the dopamine D4 re-ceptor.. Biochemistry 37 (45): 1572636.

doi:10.1021/bi981634.PMID 9843378.

Mason DA, Moore JD, Green SA, Liggett SB(1999). A gain-of-function polymorphism in aG-protein coupling domain of the human beta1-adrenergic receptor.. J. Biol. Chem. 274 (18):126704. doi:10.1074/jbc.274.18.12670. PMID10212248.

Moore JD, Mason DA, Green SA, et al. (1999).Racial differences in the frequencies of car-diac beta(1)-adrenergic receptor polymorphisms:analysis of c145A>G and c1165G>C.. Hum.

Mutat. 14 (3): 271. doi:10.1002/(SICI)1098-1004(1999)14:33.0.CO;2-Q.PMID 10477438.
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Tang Y, Hu LA, Miller WE, et al. (1999).Identification of the endophilins (SH3p4/p8/p13)as novel binding partners for the beta1-adrenergicreceptor.. Proc. Natl. Acad. Sci. U.S.A.96 (22):1255964. doi:10.1073/pnas.96.22.12559. PMC22990.PMID 10535961.

Podlowski S, Wenzel K, Luther HP, et al. (2000).Beta1-adrenoceptor gene variations: a role in idio-pathic dilated cardiomyopathy?". J. Mol. Med. 78(2): 8793. doi:10.1007/s001090000080. PMID10794544.

Shiina T, Kawasaki A, Nagao T, Kurose H(2000). Interaction with beta-arrestin deter-mines the difference in internalization behavorbetween beta1- and beta2-adrenergic recep-tors.. J. Biol. Chem. 275 (37): 2908290.doi:10.1074/jbc.M909757199.PMID 10862778.

Hu LA, Tang Y, Miller WE, et al. (2001). beta1-adrenergic receptor association with PSD-95. In-hibition of receptor internalization and facilitationof beta 1-adrenergic receptor interaction with N-methyl-D-aspartate receptors.. J. Biol. Chem. 275(49): 3865966. doi:10.1074/jbc.M005938200.PMID 10995758.

Brjesson M, Magnusson Y, Hjalmarson A, An-dersson B (2001). A novel polymorphism inthe gene coding for the beta(1)-adrenergic recep-tor associated with survival in patients with heart

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Xu J, Paquet M, Lau AG, et al. (2001). beta1-adrenergic receptor association with the synap-tic scaffolding protein membrane-associated guany-late kinase inverted-2 (MAGI-2). Differential reg-ulation of receptor internalization by MAGI-2 andPSD-95.. J. Biol. Chem. 276 (44): 413107.doi:10.1074/jbc.M107480200.PMID 11526121.

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Ranade K, Jorgenson E, Sheu WH, et al. (2002).A polymorphism in the beta1 adrenergic receptoris associated with resting heart rate.. Am. J. Hum.Genet. 70(4): 93542.doi:10.1086/339621.PMC379121.PMID 11854867.
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4 8 TEXT AND IMAGE SOURCES, CONTRIBUTORS, AND LICENSES

8 Text and image sources, contributors, and licenses

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