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
Beta-2 adrenergic receptor
Beta-3 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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4 8 TEXT AND IMAGE SOURCES, CONTRIBUTORS, AND LICENSES
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