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Beta-3 adrenergic receptor

 
Wikipedia: Beta-3 adrenergic receptor
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Adrenergic, beta-3-, receptor
Identifiers
Symbols ADRB3; BETA3AR
External IDs OMIM: 109691 MGI: 87939 HomoloGene: 37250 IUPHAR: β3-adrenoceptor
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 Q3UP63
RefSeq NM_000025 (mRNA) NM_013462 (mRNA)
NP_000016 (protein) NP_038490 (protein)
Location Chr 8:
37.94 - 37.94 Mb		 Chr 8:
28.69 - 28.7 Mb
PubMed search [1] [2]

The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is an beta-adrenergic receptor, and also denotes the human gene encoding it.[1]

Contents

Function

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]

Agonists

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

Antagonists

  • 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

Interactions

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

References

  1. ^ a b "Entrez Gene: ADRB1 adrenergic, beta-1-, receptor". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=153. 
  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. 
Stub icon This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.
v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182)
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Adrenomedullin · Anaphylatoxin (C3a, C5a) · Angiotensin (1, 2) · Apelin · Bile acid · Bombesin (BRS3, GRPR, NMBR) · Bradykinin (B1, B2) · Cannabinoid (CB1, CB2) · Chemokine · Cholecystokinin (A, B) · Dopamine (D1, D2, D3, D4, D5) · EBI2 · Endothelin (A, B) · Estrogen · Formyl peptide (1, 2, 3) · Free fatty acid (1, 2, 3, 4) · FSH · Galanin (1, 2, 3) · Gonadotropin-releasing hormone (1, 2) · GHB receptor · Ghrelin · Histamine (H1, H2, H3, H4) · Kisspeptin · Luteinizing hormone/choriogonadotropin · lysophosphatidic acid (1, 2, 3)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) · Melanocortin (1, 2, 3, 4, 5) · MCHR (1, 2) · Melatonin (1A, 1B, 1C) · Niacin (1, 2) · Motilin · Opioid (Delta, Kappa, Mu, Nociceptin & Zeta, but not Sigma) · Olfactory · Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) · Orexin (1, 2) · Oxytocin · Oxoglutarate · PAF · Prokineticin (1, 2) · Prolactin-releasing peptide · Protease-activated (1, 2, 3, 4) · Relaxin (1, 2, 3, 4) · Somatostatin (1, 2, 3, 4, 5) · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · SREB · Succinate · TAAR (1, 2, 3, 5, 6, 8, 9) · Tachykinin (1, 2, 3) · Thyrotropin · Thyrotropin-releasing hormone · Urotensin-II · Vasopressin (1A, 1B, 2)
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50)
Other
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) · Smoothened

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