Beta-1 adrenergički receptor
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Beta-1 adrenergički receptor (β1 adrenoreceptor), ili ADRB1, je beta-adrenergički receptor. ADRB1 je takođe oznaka za ljudski gen koji ga kodira.[1] On je G-protein spregnuti receptor koji vezuje Gs heterotrimerni G protein.
Receptor[uredi | uredi kod]
Dejstva[uredi | uredi kod]
Dejstva β1 receptora obuhvataju:
- stimuliše viskozne, amilazom-zasićene sekrecije pljuvačnih žlezda[2]
- Povećava srčani izlaz
- Povećava brzinu srca [3]
- Povećava kontraktilnost atrijalnog miokarda.
- Povećava kontraktilnost[3] ventrikularnog miokarda.
- Povećava provođenje[3] atrioventrikularnog čvora (AV čvor)
- Oslobađanje renina iz jukstaglomerularnih ćelija[3].
- Lipoliza u adipoznom tkivu[3].
- Receptor je takođe prisutan u cerebralnom korteksu.
Agonisti[uredi | uredi kod]
Izoprenalin ima veći afinitet za β1 od noradrenalina, koji se vezuje sa većim afinitetom od adrenalina. Selektivni agonisti beta-1 receptora su:
Antagonisti[uredi | uredi kod]
β1-selektivni antagonisti (Beta blokatori) su:
- Acebutolol (u hipertenziji, angini pektoris i aritmijama)
- Atenolol[2] (u hipertenziji, koronarnoj arterijskoj bolesti, aritmijama i srčanom udaru)
- Betaksolol (u hipertenziji i glaukomu)
- Bisoprolol[5] (u hipertenziji, koronarnoj arterijskoj bolesti, aritmijama, srčanom udaru i ishemijskom oboljenju srca)
- Esmolol (aritmije)
- Metoprolol[2] (u hipertenziji, koronarnoj arterijskoj bolesti, srčanom udaru i srčanoj insuficijenciji)
- Nebivolol (u hipertenziji)
Mehanizam[uredi | uredi kod]
Gs uzrokuje aktivaciju adenilat ciklaze, što dovodi do povećanja cAMP koncentracije.
Gen[uredi | uredi kod]
Ustanovljeno je da specifični polimorfizmi ovog gena utiču na brzinu rada srca i da mogu da imaju udela u srčanoj insuficijenciji.[1]
Interakcije[uredi | uredi kod]
Za beta-1 adrenergički receptor je pokazano da interaguje sa DLG4[6] i GIPC1.[7]
Reference[uredi | uredi kod]
- ↑ 1,0 1,1 „Entrez Gene: ADRB1 adrenergic, beta-1-, receptor”.
- ↑ 2,0 2,1 2,2 2,3 Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. str. 163. ISBN 0-443-07145-4.
- ↑ 3,0 3,1 3,2 3,3 3,4 Fitzpatrick, David; Purves, Dale; Augustine, George (2004). „Table 20:2”. Neuroscience (Third izd.). Sunderland, Mass: Sinauer. ISBN 0-87893-725-0.
- ↑ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 163
- ↑ American Society of Health-System Pharmacists, Inc. (1. 1. 2005.). „Bisoprolol”. MedlinePlus Drug Information. U.S. National Library of Medicine, National Institutes of Health. Arhivirano iz originala na datum 2008-05-20. Pristupljeno 6. 6. 2008.
- ↑ Hu, L A; Tang Y, Miller W E, Cong M, Lau A G, Lefkowitz R J, Hall R A (December 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. (UNITED STATES) 275 (49): 38659–66. DOI:10.1074/jbc.M005938200. ISSN 0021-9258. PMID 10995758.
- ↑ Hu, Liaoyuan A; Chen Wei, Martin Negin P, Whalen Erin J, Premont Richard T, Lefkowitz Robert J (July 2003). „GIPC interacts with the beta1-adrenergic receptor and regulates beta1-adrenergic receptor-mediated ERK activation”. J. Biol. Chem. (United States) 278 (28): 26295–301. DOI:10.1074/jbc.M212352200. ISSN 0021-9258. PMID 12724327.
Literatura[uredi | uredi kod]
- Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
- 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. DOI:10.1016/0166-2236(88)90095-1. 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): 1516–1520. 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): 41–8. DOI:10.1016/0022-4804(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): 7920–7924. 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 photoaffinity labeling.”. J. Biol. Chem. 258 (13): 8443–8449. 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. 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 antireceptor autoantibodies in patients with Chagas' disease.”. J. Immunol. 157 (9): 4203–4211. 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. DOI:10.1074/jbc.274.18.12670. 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: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. 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): 87–93. DOI:10.1007/s001090000080. 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): 1853–1858. 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): 1607–1613. 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. DOI:10.1086/339621. PMC 379121. PMID 11854867.
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- Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. str. 163. ISBN 0-443-07145-4.
- Fitzpatrick, David; Purves, Dale; Augustine, George (2004). „Table 20:2”. Neuroscience (Third izd.). Sunderland, Mass: Sinauer. ISBN 0-87893-725-0.
Spoljašnje veze[uredi | uredi kod]
- „β1-adrenoceptor”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2015-06-06.