Beta-1 adrenergic receptor

The beta-1 adrenergic receptor (1 adrenoreceptor), 1.3 Antagonists

also known as ADRB1, is a beta-adrenergic receptor,
and also denotes the human gene encoding it.[1] It is (Beta blockers) 1-selective ones are:
a G-protein coupled receptor associated with the Gs
heterotrimeric G-protein and is expressed predominantly
Acebutolol (in hypertension, angina pectoris and
in cardiac tissue.
arrhythmias)

Atenolol[2] (in hypertension, coronary heart disease,

arrhythmias and myocardial infarction)

Receptor

1.1

Betaxolol (in hypertension and glaucoma)

Actions

Bisoprolol[4] (in hypertension, coronary heart

disease, arrhythmias, myocardial infarction and
ischemic heart diseases)

Actions of the 1 receptor include:

Esmolol (in arrhythmias)

stimulate viscous, amylase-lled secretions from

salivary glands[2]

Metoprolol[2] (in hypertension, coronary heart disease, myocardial infarction and heart failure)

Increase cardiac output

Nebivolol (in hypertension)

Increase heart rate in sinoatrial node (SA

node) (chronotropic eect)
[3]

Vortioxetine (antidepressant)

Increase atrial cardiac muscle contractility.

1.4
(inotropic eect)

Mechanism

Increases contractility and automaticity[3] of G renders adenylate cyclase activated, resulting in inventricular cardiac muscle.
crease of cAMP.
Increases conduction and automaticity[3] of
atrioventricular node (AV node)

2 Gene

Renin release from juxtaglomerular cells.

[3]

Specic polymorphisms in the ADRB1 gene have been

shown to aect the resting heart rate and can be involved
in heart failure.[1]

Lipolysis in adipose tissue.[3]

Receptor also present in cerebral cortex.

1.2

3 Interactions

Agonists

Beta-1 adrenergic receptor has been shown to interact

Isoprenaline has higher anity for 1 than adrenaline, with DLG4[5] and GIPC1.[6] Interaction between testoswhich, in turn, binds with higher anity than terone and 1 ARs have been shown in anxiolytic benoradrenaline at physiologic concentrations. Selective haviors in the basolateral amygdala.[7]
agonists to the beta-1 receptor are:

4 See also

Denopamine
Dobutamine[2] (in cardiogenic shock)

Other adrenergic receptors

Xamoterol[2] (cardiac stimulant)

Alpha-1 adrenergic receptor

1

7 FURTHER READING
Alpha-2 adrenergic receptor
Beta-2 adrenergic receptor
Beta-3 adrenergic receptor

References

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

[2] Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill
Livingstone. ISBN 0-443-07145-4. Page 163
[3] Fitzpatrick, David; Purves, Dale; Augustine, George
(2004). Table 20:2. Neuroscience (Third ed.). Sunderland, Mass: Sinauer. ISBN 0-87893-725-0.
[4] American Society of Health-System Pharmacists, Inc.
(2005-01-01). Bisoprolol. MedlinePlus Drug Information. U.S. National Library of Medicine, National Institutes of Health. Archived from the original on 2008-0520. Retrieved 2008-06-06.
[5] Hu LA, Tang Y, Miller WE, Cong M, Lau AG, Lefkowitz
RJ, Hall RA (2000). 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): 3865966. doi:10.1074/jbc.M005938200.
PMID 10995758.
[6] Hu LA, Chen W, Martin NP, Whalen EJ, Premont
RT, Lefkowitz RJ (2003). GIPC interacts with the
beta1-adrenergic receptor and regulates beta1-adrenergic
receptor-mediated ERK activation. J. Biol. Chem. 278
(28): 26295301. doi:10.1074/jbc.M212352200. PMID
12724327.
[7] Mard-Soltani M, Kesmati M, Khajehpour L, Rasekh
A, Shamshirgar-Zadeh A (April 2012).
Interaction between Anxiolytic Eects of Testosterone and
1 Adrenoceptors of Basolateral Amygdala. International Journal of Pharmacology 8 (5): 344354.
doi:10.3923/ijp.2012.344.354.

External links
"1 -adrenoceptor. IUPHAR Database of Receptors
and Ion Channels. International Union of Basic and
Clinical Pharmacology.

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): 3214. doi:10.1016/0166-2236(88)900951. PMID 2465637.

Muszkat M (2007). Interethnic dierences in

drug response: the contribution of genetic variability in beta adrenergic receptor and cytochrome
P4502C9.. 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 receptor
genes.. Proc. Natl. Acad. Sci. U.S.A. 87 (4):
15161520. doi:10.1073/pnas.87.4.1516. PMC
53506. PMID 2154750.
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): 418. doi:10.1016/00224804(89)90180-7. PMID 2536864.
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): 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. Structural
similarities of beta 1 and beta 2 receptor subtypes
demonstrated by photoanity labeling.. J. Biol.
Chem. 258 (13): 84438449. PMID 6305985.
Hoehe MR, Otterud B, Hsieh WT, et al. (1995).
Genetic mapping of adrenergic receptor genes in
humans.. J. Mol. Med. 73 (6): 299306.
doi:10.1007/BF00231616. PMID 7583452.
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):
42034211. PMID 8892658.
Oldenhof J, Vickery R, Ana M, et al. (1998).
SH3 binding domains in the dopamine D4 receptor..
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 a
G-protein coupling domain of the human beta1adrenergic receptor.. J. Biol. Chem. 274 (18):
126704. doi:10.1074/jbc.274.18.12670. PMID
10212248.
Moore JD, Mason DA, Green SA, et al. (1999).
Racial dierences in the frequencies of cardiac beta(1)-adrenergic receptor polymorphisms:
analysis of c145A>G and c1165G>C.. Hum.
Mutat. 14 (3): 271. doi:10.1002/(SICI)10981004(1999)14:3<271::AID-HUMU14>3.0.CO;2Q. PMID 10477438.

3
Tang Y, Hu LA, Miller WE, et al. (1999).
Identication of the endophilins (SH3p4/p8/p13)
as novel binding partners for the beta1-adrenergic
receptor.. Proc. Natl. Acad. Sci. U.S.A. 96 (22):
1255964. doi:10.1073/pnas.96.22.12559. PMC
22990. PMID 10535961.
Podlowski S, Wenzel K, Luther HP, et al. (2000).
Beta1-adrenoceptor gene variations: a role in idiopathic dilated cardiomyopathy?". J. Mol. Med. 78
(2): 8793. doi:10.1007/s001090000080. PMID
10794544.
Shiina T, Kawasaki A, Nagao T, Kurose H
(2000).
Interaction with beta-arrestin determines the dierence in internalization behavor
between beta1- and beta2-adrenergic receptors.. J. Biol. Chem. 275 (37): 2908290.
doi:10.1074/jbc.M909757199. PMID 10862778.
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 Nmethyl-D-aspartate receptors.. J. Biol. Chem. 275
(49): 3865966. doi:10.1074/jbc.M005938200.
PMID 10995758.
Brjesson 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): 18531858.
doi:10.1053/euhj.1999.1994. PMID 11052857.
Xu J, Paquet M, Lau AG, et al. (2001). beta
1-adrenergic receptor association with the synaptic scaolding protein membrane-associated guanylate kinase inverted-2 (MAGI-2). Dierential regulation of receptor internalization by MAGI-2 and
PSD-95.. J. Biol. Chem. 276 (44): 413107.
doi:10.1074/jbc.M107480200. PMID 11526121.
Hu LA, Chen W, Premont RT, et al. (2002).
G protein-coupled receptor kinase 5 regulates
beta 1-adrenergic receptor association with PSD95.. J. Biol. Chem. 277 (2): 16071613.
doi:10.1074/jbc.M107297200. PMID 11700307.
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): 93542. doi:10.1086/339621. PMC
379121. PMID 11854867.

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