Beta-1 adrenergic receptor

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Adrenoceptor beta 1
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols ADRB1 ; ADRB1R; B1AR; BETA1AR; RHR
External IDs OMIM109630 MGI87937 HomoloGene20171 IUPHAR: β1-adrenoceptor ChEMBL: 213 GeneCards: ADRB1 Gene
RNA expression pattern
PBB GE ADRB1 208214 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 153 11554
Ensembl ENSG00000043591 ENSMUSG00000035283
UniProt P08588 P34971
RefSeq (mRNA) NM_000684 NM_007419
RefSeq (protein) NP_000675 NP_031445
Location (UCSC) Chr 10:
115.8 – 115.81 Mb
Chr 19:
56.72 – 56.72 Mb
PubMed search [1] [2]

The beta-1 adrenergic receptor1 adrenoreceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the human gene encoding it.[1] It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue.

Receptor[edit]

Actions[edit]

Actions of the β1 receptor include:

Agonists[edit]

Isoprenaline has higher affinity for β1 than adrenaline, which, in turn, binds with higher affinity than noradrenaline at physiologic concentrations. Selective agonists to the beta-1 receptor are:

Antagonists[edit]

(Beta blockers) β1-selective ones are:

Mechanism[edit]

Gs renders adenylate cyclase activated, resulting in increase of cAMP.

Gene[edit]

Specific polymorphisms in the ADRB1 gene have been shown to affect the resting heart rate and can be involved in heart failure.[1]

Interactions[edit]

Beta-1 adrenergic receptor has been shown to interact with DLG4[5] and GIPC1.[6] Interaction between testosterone and β-1 ARs have been shown in anxiolytic behaviors in the basolateral amygdala.[7]

See also[edit]

References[edit]

  1. ^ a b "Entrez Gene: ADRB1 adrenergic, beta-1-, receptor". 
  2. ^ a b c d e Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 163
  3. ^ a b c d e 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 2008-05-20. 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): 38659–66. 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): 26295–301. 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 Effects of Testosterone and β-1 Adrenoceptors of Basolateral Amygdala". International Journal of Pharmacology 8 (5): 344–354. doi:10.3923/ijp.2012.344.354. 

External links[edit]

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

Further reading[edit]