Beta-1 adrenergic receptor
From Wikipedia, the free encyclopedia
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]
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[edit] Receptor
[edit] 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.
[edit] Agonists
Isoprenaline has higher affinity for β1 than noradrenaline, which, in turn, binds with higher affinity than adrenaline. Selective agonists to the beta-1 receptor are:
[edit] 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)
[edit] Mechanism
Gs renders adenylate cyclase activated, resulting in increase of cAMP.
[edit] Gene
Specific polymorphisms in this gene have been shown to affect the resting heart rate and can be involved in heart failure.[1]
[edit] See also
- Other adrenergic receptors
[edit] References
- ^ a b Entrez Gene: ADRB1 adrenergic, beta-1-, receptor.
- ^ a b c d e Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 163
- ^ a b c d e Fitzpatrick, David; Purves, Dale; Augustine, George (2004). "Table 20:2", Neuroscience, Third Edition, Sunderland, Mass: Sinauer. ISBN 0-87893-725-0.
- ^ American Society of Health-System Pharmacists, Inc. (2005-01-01). Bisoprolol. MedlinePlus Drug Information. U.S. National Library of Medicine, National Institutes of Health. Retrieved on 2008-06-06.
[edit] 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. PMID 2465637.
- 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. doi: . 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): 1516–20. 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): 41–8. 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): 7920–4. 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 photoaffinity labeling.". J. Biol. Chem. 258 (13): 8443–9. PMID 6305985.
- Hoehe MR, Otterud B, Hsieh WT, et al. (1995). "Genetic mapping of adrenergic receptor genes in humans.". J. Mol. Med. 73 (6): 299–306. 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): 4203–11. PMID 8892658.
- Oldenhof J, Vickery R, Anafi M, et al. (1998). "SH3 binding domains in the dopamine D4 receptor.". Biochemistry 37 (45): 15726–36. doi: . 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 beta1-adrenergic receptor.". J. Biol. Chem. 274 (18): 12670–4. PMID 10212248.
- 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. doi: . PMID 10477438.
- 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. 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): 87–93. PMID 10794544.
- 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. doi: . 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 N-methyl-D-aspartate receptors.". J. Biol. Chem. 275 (49): 38659–66. doi: . PMID 10995758.
- 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. doi: . PMID 11052857.
- 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. doi: . PMID 11526121.
- 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. doi: . 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): 935–42. PMID 11854867.
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