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Beta-3 adrenergic receptor: Wikis


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Adrenergic, beta-3-, receptor
Symbols ADRB3; BETA3AR
External IDs OMIM109691 MGI87939 HomoloGene37250 IUPHAR: β3-adrenoceptor GeneCards: ADRB3 Gene
RNA expression pattern
PBB GE ADRB3 206812 at tn.png
PBB GE ADRB3 217303 s at tn.png
More reference expression data
Species Human Mouse
Entrez 155 11556
Ensembl ENSG00000188778 ENSMUSG00000031489
UniProt P13945 Q3UP63
RefSeq (mRNA) NM_000025 NM_013462
RefSeq (protein) NP_000016 NP_038490
Location (UCSC) Chr 8:
37.94 - 37.94 Mb
Chr 8:
28.69 - 28.7 Mb
PubMed search [1] [2]

The beta-3 adrenergic receptor3 adrenoreceptor), also known as ADRB3, is an beta-adrenergic receptor, and also denotes the human gene encoding it.[1]



Actions of the β3 receptor include:

It is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. Some β3 agonists have demonstrated antidepressant effects in animal studies, suggesting it also has a role in the CNS. Beta3-Receptors are found in the gallbladder and in brain adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat.

Mechanism of action

Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through the action of the G proteins of the type Gs.[1]


  • L-796,568[7]
  • CL-316,243[8]
  • LY-368,842
  • Ro40-2148


  • SR 59230A was thought to be a selective β3 antagonist[9] but later found to also be an antagonist of the α1 receptor.[10]

A selective β3 has potential weight loss effects through modulation of lipolysis.[2]

See also


Beta-3 adrenergic receptor has been shown to interact with Src.[11]


  1. ^ a b "Entrez Gene: ADRB1 adrenergic, beta-1-, receptor".  
  2. ^ a b 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.  
  3. ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.   Page 163
  4. ^ 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.  
  5. ^ 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.  
  6. ^ 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.  
  7. ^ 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. PMID 12324291.  
  8. ^ Fu L, Isobe K, Zeng Q, Suzukawa K, Takekoshi K, Kawakami Y. 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. 2008 Apr 14;584(1):202-6. PMID 18304529
  9. ^ 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.  
  10. ^ Bexis S, Docherty JR (April 2009). "Role of alpha(1)- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse". British Journal of Pharmacology. doi:10.1111/j.1476-5381.2009.00186.x. PMID 19422394.  
  11. ^ Cao, W; Luttrell L M, Medvedev A V, Pierce K L, Daniel K W, Dixon T M, Lefkowitz R J, Collins S (Dec. 2000). "Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation". J. Biol. Chem. (UNITED STATES) 275 (49): 38131–4. doi:10.1074/jbc.C000592200. ISSN 0021-9258. PMID 11013230.  

External links

Further reading

  • Granneman JG, Lahners KN, Rao DD (1993). "Rodent and human beta 3-adrenergic receptor genes contain an intron within the protein-coding block.". Mol. Pharmacol. 42 (6): 964–70. PMID 1336117.  
  • Nahmias C, Blin N, Elalouf JM, et al. (1991). "Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes.". EMBO J. 10 (12): 3721–7. PMID 1718744.  
  • Emorine LJ, Marullo S, Briend-Sutren MM, et al. (1989). "Molecular characterization of the human beta 3-adrenergic receptor.". Science 245 (4922): 1118–21. doi:10.1126/science.2570461. PMID 2570461.  
  • Guan XM, Amend A, Strader CD (1995). "Determination of structural domains for G protein coupling and ligand binding in beta 3-adrenergic receptor.". Mol. Pharmacol. 48 (3): 492–8. PMID 7565630.  
  • Rodriguez M, Carillon C, Coquerel A, et al. (1995). "Evidence for the presence of beta 3-adrenergic receptor mRNA in the human brain.". Brain Res. Mol. Brain Res. 29 (2): 369–75. doi:10.1016/0169-328X(94)00274-I. PMID 7609625.  
  • Clément K, Vaisse C, Manning BS, et al. (1995). "Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity.". N. Engl. J. Med. 333 (6): 352–4. doi:10.1056/NEJM199508103330605. PMID 7609752.  
  • Dib A, Adélaïde J, Chaffanet M, et al. (1995). "Characterization of the region of the short arm of chromosome 8 amplified in breast carcinoma.". Oncogene 10 (5): 995–1001. PMID 7898940.  
  • Mahmoudian M (1994). "The complex of human Gs protein with the beta 3 adrenergic receptor: a computer-aided molecular modeling study.". Journal of molecular graphics 12 (1): 22–8, 34. doi:10.1016/0263-7855(94)80004-9. PMID 8011597.  
  • Wilkie TM, Chen Y, Gilbert DJ, et al. (1994). "Identification, chromosomal location, and genome organization of mammalian G-protein-coupled receptors.". Genomics 18 (2): 175–84. doi:10.1006/geno.1993.1452. PMID 8288218.  
  • Krief S, Lönnqvist F, Raimbault S, et al. (1993). "Tissue distribution of beta 3-adrenergic receptor mRNA in man.". J. Clin. Invest. 91 (1): 344–9. doi:10.1172/JCI116191. PMID 8380813.  
  • van Spronsen A, Nahmias C, Krief S, et al. (1993). "The promoter and intron/exon structure of the human and mouse beta 3-adrenergic-receptor genes.". Eur. J. Biochem. 213 (3): 1117–24. doi:10.1111/j.1432-1033.1993.tb17861.x. PMID 8389293.  
  • Lelias JM, Kaghad M, Rodriguez M, et al. (1993). "Molecular cloning of a human beta 3-adrenergic receptor cDNA.". FEBS Lett. 324 (2): 127–30. doi:10.1016/0014-5793(93)81377-C. PMID 8389717.  
  • Candelore MR, Deng L, Tota LM, et al. (1996). "Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant.". Endocrinology 137 (6): 2638–41. doi:10.1210/en.137.6.2638. PMID 8641219.  
  • Fujisawa T, Ikegami H, Yamato E, et al. (1996). "Association of Trp64Arg mutation of the beta3-adrenergic-receptor with NIDDM and body weight gain.". Diabetologia 39 (3): 349–52. doi:10.1007/BF00418352. PMID 8721782.  
  • Higashi K, Ishikawa T, Ito T, et al. (1997). "Association of a genetic variation in the beta 3-adrenergic receptor gene with coronary heart disease among Japanese.". Biochem. Biophys. Res. Commun. 232 (3): 728–30. doi:10.1006/bbrc.1997.6339. PMID 9126344.  
  • Hoffstedt J, Poirier O, Thörne A, et al. (1999). "Polymorphism of the human beta3-adrenoceptor gene forms a well-conserved haplotype that is associated with moderate obesity and altered receptor function.". Diabetes 48 (1): 203–5. doi:10.2337/diabetes.48.1.203. PMID 9892244.  
  • Halushka MK, Fan JB, Bentley K, et al. (1999). "Patterns of single-nucleotide polymorphisms in candidate genes for blood-pressure homeostasis.". Nat. Genet. 22 (3): 239–47. doi:10.1038/10297. PMID 10391210.  
  • Kimura K, Sasaki N, Asano A, et al. (2000). "Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 preadipocytes.". Horm. Metab. Res. 32 (3): 91–6. doi:10.1055/s-2007-978597. PMID 10786926.  
  • Cao W, Luttrell LM, Medvedev AV, et al. (2001). "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.  
  • Russell ST, Hirai K, Tisdale MJ (2002). "Role of beta3-adrenergic receptors in the action of a tumour lipid mobilizing factor.". Br. J. Cancer 86 (3): 424–8. doi:10.1038/sj.bjc.6600086. PMID 11875710.  


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