Beta-3 adrenergic receptor

Beta-3 adrenergic receptor

The beta-3 adrenergic receptor3 adrenoreceptor), also known as ADRB3, is an beta-adrenergic receptor, and also denotes the human gene encoding it.cite web | title = Entrez Gene: ADRB1 adrenergic, beta-1-, receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=153| accessdate = ]

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Receptor

Functions

Actions of the β3 receptor include:
*Enhancement of lipolysis in adipose tissue.
*Thermogenesis in skeletal muscle cite book |author=Rang, H. P. |title=Pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2003 |pages= |isbn=0-443-07145-4 |oclc= |doi= Page 163 ]

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.

Mechanism

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.cite web | title = Entrez Gene: ADRB3 adrenergic, beta-3-, receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=155| accessdate = ]

Agonists

* Amibegron (SR-58611A) [Consoli D, Leggio GM, Mazzola C, Micale V, Drago F. Behavioral effects of the beta3 adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs? "European Journal of Pharmacology". 2007 Nov 14;573(1-3):139-47. PMID 17669397] [Overstreet DH, Stemmelin J, Griebel G. Confirmation of antidepressant potential of the selective beta3 adrenoceptor agonist amibegron in an animal model of depression. "Pharmacology, Biochemistry and Behaviour". 2008 Jun;89(4):623-6. PMID 18358519]
* Solabegron (GW-427,353) [Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C, Luce TD, Coatney RW, Rivera GC, Westfall TD, Hieble JP. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. "Journal of Pharmacology and Experimental Therapeutics". 2007 Oct;323(1):202-9. PMID 17626794]
* L-796,568cite journal | author = Larsen TM, Toubro S, van Baak MA, Gottesdiener KM, Larson P, Saris WH, Astrup A | title = Effect of a 28-d treatment with L-796568, a novel β3-adrenergic receptor agonist, on energy expenditure and body composition in obese men | journal = Am. J. Clin. Nutr. | volume = 76 | issue = 4 | pages = 780–8 | year = 2002 | pmid = 12324291 | doi = | issn = ]
* CL-316,243 [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]
* LY-368,842
* Ro40-2148

Antagonists

* SR 59230A cite journal | author = Nisoli E, Tonello C, Landi M, Carruba MO | title = Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes | journal = Mol. Pharmacol. | volume = 49 | issue = 1 | pages = 7–14 | year = 1996 | pmid = 8569714 | doi = | issn = ]

ee also

*Other adrenergic receptors
**Alpha-1 adrenergic receptor
**Alpha-2 adrenergic receptor
**Beta-1 adrenergic receptor
**Beta-2 adrenergic receptor

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=Granneman JG, Lahners KN, Rao DD |title=Rodent and human beta 3-adrenergic receptor genes contain an intron within the protein-coding block. |journal=Mol. Pharmacol. |volume=42 |issue= 6 |pages= 964–70 |year= 1993 |pmid= 1336117 |doi=
*cite journal | author=Nahmias C, Blin N, Elalouf JM, "et al." |title=Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes. |journal=EMBO J. |volume=10 |issue= 12 |pages= 3721–7 |year= 1991 |pmid= 1718744 |doi=
*cite journal | author=Emorine LJ, Marullo S, Briend-Sutren MM, "et al." |title=Molecular characterization of the human beta 3-adrenergic receptor. |journal=Science |volume=245 |issue= 4922 |pages= 1118–21 |year= 1989 |pmid= 2570461 |doi=
*cite journal | author=Guan XM, Amend A, Strader CD |title=Determination of structural domains for G protein coupling and ligand binding in beta 3-adrenergic receptor. |journal=Mol. Pharmacol. |volume=48 |issue= 3 |pages= 492–8 |year= 1995 |pmid= 7565630 |doi=
*cite journal | author=Rodriguez M, Carillon C, Coquerel A, "et al." |title=Evidence for the presence of beta 3-adrenergic receptor mRNA in the human brain. |journal=Brain Res. Mol. Brain Res. |volume=29 |issue= 2 |pages= 369–75 |year= 1995 |pmid= 7609625 |doi=
*cite journal | author=Clément K, Vaisse C, Manning BS, "et al." |title=Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity. |journal=N. Engl. J. Med. |volume=333 |issue= 6 |pages= 352–4 |year= 1995 |pmid= 7609752 |doi=
*cite journal | author=Dib A, Adélaïde J, Chaffanet M, "et al." |title=Characterization of the region of the short arm of chromosome 8 amplified in breast carcinoma. |journal=Oncogene |volume=10 |issue= 5 |pages= 995–1001 |year= 1995 |pmid= 7898940 |doi=
*cite journal | author=Mahmoudian M |title=The complex of human Gs protein with the beta 3 adrenergic receptor: a computer-aided molecular modeling study. |journal=Journal of molecular graphics |volume=12 |issue= 1 |pages= 22–8, 34 |year= 1994 |pmid= 8011597 |doi=
*cite journal | author=Wilkie TM, Chen Y, Gilbert DJ, "et al." |title=Identification, chromosomal location, and genome organization of mammalian G-protein-coupled receptors. |journal=Genomics |volume=18 |issue= 2 |pages= 175–84 |year= 1994 |pmid= 8288218 |doi= 10.1006/geno.1993.1452
*cite journal | author=Krief S, Lönnqvist F, Raimbault S, "et al." |title=Tissue distribution of beta 3-adrenergic receptor mRNA in man. |journal=J. Clin. Invest. |volume=91 |issue= 1 |pages= 344–9 |year= 1993 |pmid= 8380813 |doi=
*cite journal | author=van Spronsen A, Nahmias C, Krief S, "et al." |title=The promoter and intron/exon structure of the human and mouse beta 3-adrenergic-receptor genes. |journal=Eur. J. Biochem. |volume=213 |issue= 3 |pages= 1117–24 |year= 1993 |pmid= 8389293 |doi=
*cite journal | author=Lelias JM, Kaghad M, Rodriguez M, "et al." |title=Molecular cloning of a human beta 3-adrenergic receptor cDNA. |journal=FEBS Lett. |volume=324 |issue= 2 |pages= 127–30 |year= 1993 |pmid= 8389717 |doi=
*cite journal | author=Candelore MR, Deng L, Tota LM, "et al." |title=Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant. |journal=Endocrinology |volume=137 |issue= 6 |pages= 2638–41 |year= 1996 |pmid= 8641219 |doi=
*cite journal | author=Fujisawa T, Ikegami H, Yamato E, "et al." |title=Association of Trp64Arg mutation of the beta3-adrenergic-receptor with NIDDM and body weight gain. |journal=Diabetologia |volume=39 |issue= 3 |pages= 349–52 |year= 1996 |pmid= 8721782 |doi=
*cite journal | author=Higashi K, Ishikawa T, Ito T, "et al." |title=Association of a genetic variation in the beta 3-adrenergic receptor gene with coronary heart disease among Japanese. |journal=Biochem. Biophys. Res. Commun. |volume=232 |issue= 3 |pages= 728–30 |year= 1997 |pmid= 9126344 |doi= 10.1006/bbrc.1997.6339
*cite journal | author=Hoffstedt J, Poirier O, Thörne A, "et al." |title=Polymorphism of the human beta3-adrenoceptor gene forms a well-conserved haplotype that is associated with moderate obesity and altered receptor function. |journal=Diabetes |volume=48 |issue= 1 |pages= 203–5 |year= 1999 |pmid= 9892244 |doi=
*cite journal | author=Halushka MK, Fan JB, Bentley K, "et al." |title=Patterns of single-nucleotide polymorphisms in candidate genes for blood-pressure homeostasis. |journal=Nat. Genet. |volume=22 |issue= 3 |pages= 239–47 |year= 1999 |pmid= 10391210 |doi= 10.1038/10297
*cite journal | author=Kimura K, Sasaki N, Asano A, "et al." |title=Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 preadipocytes. |journal=Horm. Metab. Res. |volume=32 |issue= 3 |pages= 91–6 |year= 2000 |pmid= 10786926 |doi=
*cite journal | author=Cao W, Luttrell LM, Medvedev AV, "et al." |title=Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation. |journal=J. Biol. Chem. |volume=275 |issue= 49 |pages= 38131–4 |year= 2001 |pmid= 11013230 |doi= 10.1074/jbc.C000592200
*cite journal | author=Russell ST, Hirai K, Tisdale MJ |title=Role of beta3-adrenergic receptors in the action of a tumour lipid mobilizing factor. |journal=Br. J. Cancer |volume=86 |issue= 3 |pages= 424–8 |year= 2002 |pmid= 11875710 |doi= 10.1038/sj.bjc.6600086

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