Beta-3 adrenergic receptor

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Adrenoceptor beta 3
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols ADRB3 ; BETA3AR
External IDs OMIM109691 MGI87939 HomoloGene37250 IUPHAR: β3-adrenoceptor ChEMBL: 246 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
Orthologs
Species Human Mouse
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:
37.82 – 37.82 Mb
Chr 8:
27.23 – 27.23 Mb
PubMed search [1] [2]

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

Function[edit]

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 antistress effects in animal studies, suggesting it also has a role in the central nervous system (CNS). Beta3-Receptors are found in the gallbladder, urinary bladder, and in brown 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.[4]

Mechanism of action[edit]

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]

Ligands[edit]

Agonists[edit]

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

Antagonists[edit]

Interactions[edit]

Beta-3 adrenergic receptor has been shown to interact with Src.[14]

See also[edit]

References[edit]

  1. ^ a b "Entrez Gene: ADRB3 adrenergic, beta-3-, 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.  Vancouver style error (help)
  3. ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 163
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ a b c Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y et al. (Aug 1999). "Potent and selective human beta(3)-adrenergic receptor antagonists.". The Journal of Pharmacology and Experimental Therapeutics 290 (2): 649–55. PMID 10411574. 
  9. ^ Larsen TM, Toubro S, van Baak MA, Gottesdiener KM, Larson P, Saris WH et al. (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. 
  10. ^ Gras J (2012). "Mirabegron for the treatment of overactive bladder". Drugs of today (Barcelona, Spain : 1998) 48 (1): 25–32. doi:10.1358/dot.2012.48.1.1738056. PMID 22384458. 
  11. ^ Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C et al. (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. 
  12. ^ 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. 
  13. ^ 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. 
  14. ^ Cao W, Luttrell LM, Medvedev AV, Pierce KL, Daniel KW, Dixon TM et al. (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[edit]

  • 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, Mattei MG, Strosberg AD, Emorine LJ (1991). "Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes". EMBO J. 10 (12): 3721–7. PMC 453106. PMID 1718744. 
  • Emorine LJ, Marullo S, Briend-Sutren MM, Patey G, Tate K, Delavier-Klutchko C 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, Le Fur G, Ferrara P, Caput D 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, Basdevant A, Guy-Grand B, Ruiz J 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.  Vancouver style error (help)
  • Dib A, Adélaïde J, Chaffanet M, Imbert A, Le Paslier D, Jacquemier J 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.  Vancouver style error (help)
  • 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, Moore KJ, Yu L, Simon MI 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, Baude B, Van Spronsen A, Arner P et al. (1993). "Tissue distribution of beta 3-adrenergic receptor mRNA in man". J. Clin. Invest. 91 (1): 344–9. doi:10.1172/JCI116191. PMC 330032. PMID 8380813.  Vancouver style error (help)
  • van Spronsen A, Nahmias C, Krief S, Briend-Sutren MM, Strosberg AD, Emorine LJ (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, Chalon P, Bonnin J, Dupre I 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, Kelly LJ, Cascieri MA, Strader CD (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, Takekawa K, Nakagawa Y, Hamada Y 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, Yonemura A, Shige H, Nakamura H (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, Lönnqvist F, Herrmann SM, Cambien F 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.  Vancouver style error (help)
  • Halushka MK, Fan JB, Bentley K, Hsie L, Shen N, Weder A 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, Mizukami J, Kayahashi S, Kawada T 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, Pierce KL, Daniel KW, Dixon TM 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 β3-adrenergic receptors in the action of a tumour lipid mobilizing factor". Br. J. Cancer 86 (3): 424–8. doi:10.1038/sj.bjc.6600086. PMC 2375201. PMID 11875710. 

External links[edit]

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