Beta-1 adrenergic receptor

	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 · Neuroscience · Psychoneuroimmunology · Physiological Psychology · Psychopharmacology (Index, Outline)

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]

Receptor[]

Actions[]

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.

Agonists[]

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)

Antagonists[]

(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)

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.^[1]

References[]

↑ ^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 reading[]

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

[Rang163-2] 2.0 ^2.1 ^2.2 ^2.3 ^2.4 Rang, H. P. (2003). Pharmacology, Edinburgh: Churchill Livingstone. Page 163

[purves-3] 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-4] Bisoprolol MedlinePlus

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