Beta-1 adrenergic receptor
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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]
Contents |
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, binds with higher affinity than adrenaline. Selective agonists to the beta-1 receptor are:
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
Gs 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]
See also
- Other adrenergic receptors
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. ISBN 0-443-07145-4. 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. ISBN 0-87893-725-0.
- ↑ 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. 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: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): 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: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 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:<271::AID-HUMU14>3.0.CO;2-Q 10.1002/(SICI)1098-1004(1999)14:3<271::AID-HUMU14>3.0.CO;2-Q. 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: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 N-methyl-D-aspartate receptors.". J. Biol. Chem. 275 (49): 38659-66. doi:10.1074/jbc.M005938200. 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:10.1053/euhj.1999.1994. 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: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 PSD-95.". J. Biol. Chem. 277 (2): 1607-13. 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): 935-42. PMID 11854867.
Template:Membrane-protein-stub
Transmembrane receptor: G protein-coupled receptors | |
|---|---|
| Class A: Rhodopsin like | Acetylcholine (M1, M2, M3, M4, M5) - Adrenergic (α1 (A, B, D), α2 (A, B, C), β1, β2, β3) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - Eicosanoid (CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin ((DP (1, 2), EP (1, 2, 3, 4), PGF, Prostacyclin, Thromboxane) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 182) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - Neuromedin (B, U (1, 2)) - Neuropeptide (B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Purinergics (Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - Serotonin, all but 5-HT3 (5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2) |
| Class B: Secretin like | Brain-specific angiogenesis inhibitor (1, 2, 3) - Cadherin (1, 2, 3) - Calcitonin - CD97 - Corticotropin-releasing hormone (1, 2) - EMR (1, 2, 3) - Glucagon (GR, GIPR, GLP1R, GLP2R) - Growth hormone releasing hormone - PACAPR1- GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157) - Latrophilin (1, 2, 3, ELTD1) - Parathyroid hormone (1, 2) - Secretin - Vasoactive intestinal peptide (1, 2) |
| Class C: Metabotropic glutamate / pheromone | Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50)) |
| Frizzled / Smoothened | Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened |
| ||||
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
