Wikia

	Adrenergic, beta-1-, receptor
	Identifiers
Symbol(s)	ADRB1; ADRB1R; B1AR; BETA1AR; RHR
External IDs	OMIM: 109630 MGI: 87937 Homologene: 20171
Gene Ontology
Molecular Function:	• rhodopsin-like receptor activity; • receptor activity; • adrenoceptor activity; • beta1-adrenergic receptor activity; • protein binding;
Cellular Component:	• membrane fraction; • plasma membrane; • integral to plasma membrane; • membrane; • integral to membrane;
Biological Process:	• positive regulation of heart contraction rate by epinephrine-norepinephrine; • increased strength of heart contraction by epinephrine-norepinephrine; • diet induced thermogenesis; • norepinephrine-epinephrine vasodilation during regulation of blood pressure; • signal transduction; • G-protein coupled receptor protein signaling pathway; • adenylate cyclase activation; • response to cold; • heat generation; • negative regulation of body size; • fear response; • brown fat cell differentiation;
	Orthologs

Biological: Behavioural genetics · Evolutionary psychology · Neuroanatomy · Neurochemistry · Neuroendocrinology · Psychoneuroimmunology · Physiological Psychology · Psychopharmacology

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

ReceptorEdit

ActionsEdit

Actions of the β₁ receptor include:

stimulate viscous, amylase-filled secretions from salivary glands^[2]
Increase cardiac output
- Increase heart rate ^[3] in sinoatrial node (SA node) (chronotropic effect)
- Increase atrial cardiac muscle contractility. (inotropic effect)
- Increases contractility and automaticity^[3] of ventricular cardiac muscle.
- Increases conduction and automaticity^[3] of atrioventricular node (AV node)

Renin release from juxtaglomerular cells^[3].
Lipolysis in adipose tissue^[3].
Receptor also present in cerebral cortex.

AgonistsEdit

isoprenaline has higher affinity for β₁ than noradrenaline, which, in turn, bind with higher affinity than adrenaline. Selective agonists to the beta-1 receptor are:

dobutamine^[2] (in cardiogenic shock)
xamoterol^[2] (cardiac stimulant)

AntagonistsEdit

(Beta blockers) β1-selective ones are:

Acebutolol (in hypertension, angina pectoris and arrhythmias)
Atenolol^[2] (in hypertension, coronary heart disease, arrhythmias and myocardial infarction)
Betaxolol (in hypertension and glaucoma)
Bisoprolol^[4] (in hypertension, coronary heart disease, arrhythmias, myocardial infarction and ischemic heart diseases)
Esmolol (in arrhythmias)
Metoprolol^[2] (in hypertension, coronary heart disease, myocardial infarction and heart failure)
Nebivolol (in hypertension)

MechanismEdit

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

GeneEdit

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

ReferencesEdit

↑ ^1.0 ^1.1 Entrez Gene: ADRB1 adrenergic, beta-1-, receptor.
↑ ^2.0 ^2.1 ^2.2 ^2.3 ^2.4 Rang, H. P. (2003). Pharmacology, Edinburgh: Churchill Livingstone. Page 163
↑ ^3.0 ^3.1 ^3.2 ^3.3 ^3.4 Fitzpatrick, David; Purves, Dale; Augustine, George (2004). "Table 20:2" Neuroscience, Third Edition, Sunderland, Mass: Sinauer.
↑ Bisoprolol MedlinePlus

Further readingEdit

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

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[entrez-0] 1.0 ^1.1 Entrez Gene: ADRB1 adrenergic, beta-1-, receptor.

[Rang163-1] 2.0 ^2.1 ^2.2 ^2.3 ^2.4 Rang, H. P. (2003). Pharmacology, Edinburgh: Churchill Livingstone. Page 163

[purves-2] 3.0 ^3.1 ^3.2 ^3.3 ^3.4 Fitzpatrick, David; Purves, Dale; Augustine, George (2004). "Table 20:2" Neuroscience, Third Edition, Sunderland, Mass: Sinauer.

[bisoprolol-3] Bisoprolol MedlinePlus

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Wikia

Beta-1 adrenergic receptor

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