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Beta-3 adrenergic receptor

From Wikipedia, the free encyclopedia
Mammalian protein found in Homo sapiens

ADRB3
Available structures
PDBOrtholog search:PDBeRCSB
List of PDB id codes

2CDW

Identifiers
AliasesADRB3, BETA3AR, adrenoceptor beta 3
External IDsOMIM:109691;MGI:87939;HomoloGene:37250;GeneCards:ADRB3;OMA:ADRB3 - orthologs
Gene location (Human)
Chromosome 8 (human)
Chr.Chromosome 8 (human)[1]
Chromosome 8 (human)
Genomic location for ADRB3
Genomic location for ADRB3
Band8p11.23Start37,962,990bp[1]
End37,966,599bp[1]
Gene location (Mouse)
Chromosome 8 (mouse)
Chr.Chromosome 8 (mouse)[2]
Chromosome 8 (mouse)
Genomic location for ADRB3
Genomic location for ADRB3
Band8 A2|8 15.94 cMStart27,225,776bp[2]
End27,250,616bp[2]
RNA expression pattern
Bgee
HumanMouse (ortholog)
Top expressed in
  • right ovary

  • left ovary

  • testicle

  • left uterine tube

  • placenta

  • urinary bladder

  • gallbladder

  • gonad

  • muscle layer of sigmoid colon

  • fundus
Top expressed in
  • lactiferous gland

  • white adipose tissue

  • brown adipose tissue

  • tunica adventitia of aorta

  • subcutaneous adipose tissue

  • intercostal muscle

  • tunica media of zone of aorta

  • trachea

  • mesenteric lymph nodes

  • embryo
More reference expression data
BioGPS


More reference expression data
Gene ontology
Molecular function
Cellular component
Biological process
Sources:Amigo /QuickGO
Orthologs
SpeciesHumanMouse
Entrez

155

11556

Ensembl

ENSG00000188778

ENSMUSG00000031489

UniProt

P13945

P25962

RefSeq (mRNA)

NM_000025

NM_013462

RefSeq (protein)

NP_000016

NP_038490

Location (UCSC)Chr 8: 37.96 – 37.97 MbChr 8: 27.23 – 27.25 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Thebeta-3 adrenergic receptor (β3-adrenoceptor), also known asADRB3, is abeta-adrenergic receptor, and also denotes the humangene encoding it.[5]

Function

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Actions of the β3 receptor include

It is located mainly inadipose tissue and is involved in the regulation of lipolysis andthermogenesis. Some β3agonists have demonstratedantistress effects in animal studies, suggesting it also has a role in the central nervous system (CNS). β3 receptors are found in the gallbladder, urinary bladder, and inbrown adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat. In the urinary bladder it is thought to cause relaxation of the bladder and prevention of urination.[8]

Mechanism of action

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Beta adrenergic receptors are involved in theepinephrine- andnorepinephrine-induced activation ofadenylate cyclase through the action of theG proteins of the typeGs.[5]

Ligands

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Agonists

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Approved for clinical use

[edit]
  • Mirabegron (YM-178),[9] approved for treatment of overactive bladder in Japan, United States, UK, Canada, China and India.
  • Nebivolol[10] selective beta(1)-blocker and beta(3)-agonist.
  • Vibegron (MK-4618)[11]

Experimental

[edit]

Antagonists

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Interactions

[edit]

Beta-3 adrenergic receptor has been shown tointeract withSrc.[21]

See also

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References

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  1. ^abcGRCh38: Ensembl release 89: ENSG00000188778Ensembl, May 2017
  2. ^abcGRCm38: Ensembl release 89: ENSMUSG00000031489Ensembl, May 2017
  3. ^"Human PubMed Reference:".National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^"Mouse PubMed Reference:".National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ab"Entrez Gene: ADRB3 adrenergic, beta-3-, receptor".
  6. ^Ferrer-Lorente R, Cabot C, Fernández-López JA, Alemany M (September 2005)."Combined effects of oleoyl-estrone and a β3-adrenergic agonist (CL316,243) on lipid stores of diet-induced overweight male Wistar rats".Life Sciences.77 (16):2051–8.doi:10.1016/j.lfs.2005.04.008.PMID 15935402.
  7. ^Rang, H. P. (2003).Pharmacology. Edinburgh: Churchill Livingstone.ISBN 0-443-07145-4. Page 163
  8. ^Sawa M, Harada H (2006). "Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists".Current Medicinal Chemistry.13 (1):25–37.doi:10.2174/092986706775198006.PMID 16457637.
  9. ^Gras J (2012). "Mirabegron for the treatment of overactive bladder".Drugs of Today.48 (1):25–32.doi:10.1358/dot.2012.48.1.1738056.PMID 22384458.
  10. ^Rozec B, Erfanian M, Laurent K, Trochu JN, Gauthier C (2009). "Nebivolol, a vasodilating selective beta(1)-blocker, is a beta(3)-adrenoceptor agonist in the nonfailing transplanted human heart".J Am Coll Cardiol.53 (17):1532–8.doi:10.1016/j.jacc.2008.11.057.PMID 19389564.
  11. ^Edmondson SD, Zhu C, Kar NF, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen DM, Wang L, Ball R, Fitzmaurice A, Frenkl T, Gichuru LN, Ha S, Hurley AL, Jochnowitz N, Levorse D, Mistry S, Miller RR, Ormes J, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Green S, Struthers M, Weber AE (January 2016). "Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder".Journal of Medicinal Chemistry.59 (2):609–23.doi:10.1021/acs.jmedchem.5b01372.PMID 26709102.
  12. ^Consoli D, Leggio GM, Mazzola C, Micale V, Drago F (November 2007). "Behavioral effects of the β3 adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs?".European Journal of Pharmacology.573 (1–3):139–47.doi:10.1016/j.ejphar.2007.06.048.PMID 17669397.
  13. ^Overstreet DH, Stemmelin J, Griebel G (June 2008). "Confirmation of antidepressant potential of the selective β3 adrenoceptor agonist amibegron in an animal model of depression".Pharmacology Biochemistry and Behavior.89 (4):623–6.doi:10.1016/j.pbb.2008.02.020.PMID 18358519.S2CID 35026036.
  14. ^Mukaida S, Sato M, Öberg AI, Dehvari N, Olsen JM, Kocan M, et al. (May 2019)."BRL37344 stimulates GLUT4 translocation and glucose uptake in skeletal muscle via β2-adrenoceptors without causing classical receptor desensitization".American Journal of Physiology. Regulatory, Integrative and Comparative Physiology.316 (5):R666 –R677.doi:10.1152/ajpregu.00285.2018.PMID 30892909.
  15. ^Fu L, Isobe K, Zeng Q, Suzukawa K, Takekoshi K, Kawakami Y (2008). "The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice".European Journal of Pharmacology.584 (1):202–6.doi:10.1016/j.ejphar.2008.01.028.PMID 18304529.
  16. ^abcCandelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, Cascieri MA, Weber AE (August 1999). "Potent and selective human beta(3)-adrenergic receptor antagonists".The Journal of Pharmacology and Experimental Therapeutics.290 (2):649–55.PMID 10411574.
  17. ^Larsen TM, Toubro S, van Baak MA, Gottesdiener KM, Larson P, Saris WH, Astrup A (2002)."Effect of a 28-d treatment with L-796568, a novel β3-adrenergic receptor agonist, on energy expenditure and body composition in obese men".The American Journal of Clinical Nutrition.76 (4):780–8.doi:10.1093/ajcn/76.4.780.PMID 12324291.
  18. ^Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C, Luce TD, Coatney RW, Rivera GC, Westfall TD, Hieble JP (October 2007). "GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog".The Journal of Pharmacology and Experimental Therapeutics.323 (1):202–9.doi:10.1124/jpet.107.125757.PMID 17626794.S2CID 19281697.
  19. ^Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes".Mol. Pharmacol.49 (1):7–14.PMID 8569714.
  20. ^Bexis S, Docherty JR (April 2009)."Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse".British Journal of Pharmacology.158 (1):259–66.doi:10.1111/j.1476-5381.2009.00186.x.PMC 2795232.PMID 19422394.
  21. ^Cao W, Luttrell LM, Medvedev AV, Pierce KL, Daniel KW, Dixon TM, Lefkowitz RJ, Collins S (2000)."Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation".J. Biol. Chem.275 (49):38131–4.doi:10.1074/jbc.C000592200.PMID 11013230.

Further reading

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External links

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