Beta-3 adrenergic receptor: Difference between revisions

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{{Infobox_gene}}
The '''beta-3 adrenergic receptor''' (β<sub>3</sub> adrenoreceptor), also known as '''ADRB3''', is a [[beta-adrenergic receptor]], and also denotes the human [[gene]] encoding it.<ref name="entrez">{{cite web | title = Entrez Gene: ADRB3 adrenergic, beta-3-, receptor| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=155| accessdate = }}</ref>


== Function ==


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Actions of the β<sub>3</sub> receptor include
{{PBB_Controls
*Enhancement of [[lipolysis]] in [[adipose tissue]].<ref name="pmid15935402">{{cite journal | vauthors = Ferrer-Lorente R, Cabot C, Fernández-López JA, Alemany M | title = Combined effects of oleoyl-estrone and a β<sub>3</sub>-adrenergic agonist (CL316,243) on lipid stores of diet-induced overweight male Wistar rats | journal = Life Sciences | volume = 77 | issue = 16 | pages = 2051–8 | date = September 2005 | pmid = 15935402 | doi = 10.1016/j.lfs.2005.04.008 }}</ref>
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*[[Thermogenesis]] in [[skeletal muscle]]<ref name=Rang163>{{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</ref>
| require_manual_inspection = no
| update_protein_box = yes
| update_summary = no
| update_citations = yes
}}


<!-- The GNF_Protein_box is automatically maintained by Protein Box Bot. See Template:PBB_Controls to Stop updates. -->
It is located mainly in [[adipose tissue]] and is involved in the regulation of lipolysis and [[thermogenesis]]. Some β<sub>3</sub> [[agonist]]s have demonstrated [[antistress]] effects in animal studies, suggesting it also has a role in the central nervous system (CNS). β<sub>3</sub> 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.<ref name="pmid16457637">{{cite journal | vauthors = Sawa M, Harada H | title = Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists | journal = Current Medicinal Chemistry | volume = 13 | issue = 1 | pages = 25–37 | year = 2006 | pmid = 16457637 | doi = 10.2174/092986706775198006 }}</ref>
{{GNF_Protein_box
| image = 
| image_source = 
| PDB =
| Name = Adrenergic, beta-3-, receptor
| HGNCid = 288
| Symbol = ADRB3
| AltSymbols =; BETA3AR
| OMIM = 109691
| ECnumber = 
| Homologene = 37250
| MGIid = 87939
| GeneAtlas_image1 = PBB_GE_ADRB3_206812_at_tn.png
| GeneAtlas_image2 = PBB_GE_ADRB3_217303_s_at_tn.png
| Function = {{GNF_GO|id=GO:0001584 |text = rhodopsin-like receptor activity}} {{GNF_GO|id=GO:0004872 |text = receptor activity}} {{GNF_GO|id=GO:0015052 |text = beta3-adrenergic receptor activity}} {{GNF_GO|id=GO:0031699 |text = beta-3 adrenergic receptor binding}} {{GNF_GO|id=GO:0042803 |text = protein homodimerization activity}} {{GNF_GO|id=GO:0051380 |text = norepinephrine binding}}
| Component = {{GNF_GO|id=GO:0005624 |text = membrane fraction}} {{GNF_GO|id=GO:0005886 |text = plasma membrane}} {{GNF_GO|id=GO:0005887 |text = integral to plasma membrane}} {{GNF_GO|id=GO:0043235 |text = receptor complex}}
| Process = {{GNF_GO|id=GO:0002024 |text = diet induced thermogenesis}} {{GNF_GO|id=GO:0002025 |text = norepinephrine-epinephrine vasodilation during regulation of blood pressure}} {{GNF_GO|id=GO:0002032 |text = arrestin mediated desensitization of G-protein coupled receptor protein signaling pathway}} {{GNF_GO|id=GO:0005975 |text = carbohydrate metabolic process}} {{GNF_GO|id=GO:0006091 |text = generation of precursor metabolites and energy}} {{GNF_GO|id=GO:0006112 |text = energy reserve metabolic process}} {{GNF_GO|id=GO:0006898 |text = receptor-mediated endocytosis}} {{GNF_GO|id=GO:0007165 |text = signal transduction}} {{GNF_GO|id=GO:0007190 |text = adenylate cyclase activation}} {{GNF_GO|id=GO:0009409 |text = response to cold}} {{GNF_GO|id=GO:0031649 |text = heat generation}} {{GNF_GO|id=GO:0040015 |text = negative regulation of body size}} {{GNF_GO|id=GO:0043410 |text = positive regulation of MAPKKK cascade}} {{GNF_GO|id=GO:0050873 |text = brown fat cell differentiation}}
| Orthologs = {{GNF_Ortholog_box
    | Hs_EntrezGene = 155
    | Hs_Ensembl = ENSG00000188778
    | Hs_RefseqProtein = NP_000016
    | Hs_RefseqmRNA = NM_000025
    | Hs_GenLoc_db = 
    | Hs_GenLoc_chr = 8
    | Hs_GenLoc_start = 37939673
    | Hs_GenLoc_end = 37943341
    | Hs_Uniprot = P13945
    | Mm_EntrezGene = 11556
    | Mm_Ensembl = ENSMUSG00000031489
    | Mm_RefseqmRNA = NM_013462
    | Mm_RefseqProtein = NP_038490
    | Mm_GenLoc_db = 
    | Mm_GenLoc_chr = 8
    | Mm_GenLoc_start = 28691712
    | Mm_GenLoc_end = 28695524
    | Mm_Uniprot = Q3UP63
  }}
}}
The '''beta-3 adrenergic receptor''' (β<sub>3</sub> adrenoreceptor), also known as '''ADRB3''', is an [[beta-adrenergic receptor]], and also denotes the human [[gene]] encoding it.<ref name="entrez">{{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 = }}</ref>


<!-- The PBB_Summary template is not automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Continue updates. -->
== Mechanism of action ==
{{PBB_Summary
| section_title =  
| summary_text =  
}}


==Receptor==
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 alpha subunit|G<sub>s</sub>]].<ref name="entrez"/>
===Functions===
Actions of the β<sub>3</sub> receptor include:
*Enhancement of [[lipolysis]] in [[adipose tissue]].
*[[Thermogenesis]] in [[skeletal muscle]]<ref name=Rang163> {{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 </ref>


It is located mainly in [[adipose tissue]] and is involved in the regulation of lipolysis and [[thermogenesis]].
== Ligands ==


===Mechanism===
=== Agonists ===
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 alpha subunit|G<sub>s</sub>]].<ref name="entrez">{{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 = }}</ref>


==Agonists==
* [[Amibegron]] (SR-58611A)<ref name="pmid17669397">{{cite journal | vauthors = Consoli D, Leggio GM, Mazzola C, Micale V, Drago F | title = Behavioral effects of the β<sub>3</sub> adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs? | journal = European Journal of Pharmacology | volume = 573 | issue = 1–3 | pages = 139–47 | date = November 2007 | pmid = 17669397 | doi = 10.1016/j.ejphar.2007.06.048 }}</ref><ref name="pmid18358519">{{cite journal | vauthors = Overstreet DH, Stemmelin J, Griebel G | title = Confirmation of antidepressant potential of the selective β<sub>3</sub> adrenoceptor agonist amibegron in an animal model of depression | journal = Pharmacology, Biochemistry, and Behavior | volume = 89 | issue = 4 | pages = 623–6 | date = June 2008 | pmid = 18358519 | doi = 10.1016/j.pbb.2008.02.020 }}</ref>
*L-796568<ref name="pmid12324291">{{cite 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 β<sub>3</sub>-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 = }}</ref>
* CL-316,243<ref>{{cite journal | vauthors = Fu L, Isobe K, Zeng Q, Suzukawa K, Takekoshi K, Kawakami Y | title = 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 | journal = European Journal of Pharmacology | volume = 584 | issue = 1 | pages = 202–6 | year = 2008 | pmid = 18304529 | doi = 10.1016/j.ejphar.2008.01.028 }}</ref>
*CL 316,243
* L-742,791<ref name="pmid10411574">{{cite journal | vauthors = Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, Cascieri MA, Weber AE | title = Potent and selective human beta(3)-adrenergic receptor antagonists. | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 290 | issue = 2 | pages = 649–55 | date = Aug 1999 | pmid = 10411574 }}</ref>
*LY 368842
* L-796,568<ref name="pmid12324291">{{cite journal | vauthors = 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 β<sub>3</sub>-adrenergic receptor agonist, on energy expenditure and body composition in obese men | journal = The American Journal of Clinical Nutrition | volume = 76 | issue = 4 | pages = 780–8 | year = 2002 | pmid = 12324291 | doi = }}</ref>
*Ro 40-2148
* LY-368,842
* [[Mirabegron]] (YM-178),<ref>{{cite journal | vauthors = Gras J | title = Mirabegron for the treatment of overactive bladder | journal = Drugs of today (Barcelona, Spain : 1998) | volume = 48 | issue = 1 | pages = 25–32 | year = 2012 | pmid = 22384458 | doi = 10.1358/dot.2012.48.1.1738056 }}</ref> approved for treatment of overactive bladder in Japan, United States, UK, Canada, China and India.
* Ro40-2148
* [[Solabegron]] (GW-427,353)<ref name="pmid17626794">{{cite journal | vauthors = Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C, Luce TD, Coatney RW, Rivera GC, Westfall TD, Hieble JP | title = GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 323 | issue = 1 | pages = 202–9 | date = October 2007 | pmid = 17626794 | doi = 10.1124/jpet.107.125757 }}</ref>
* [[Vibegron]] (MK-4618)<ref name="pmid17626795">{{cite journal | vauthors = Edmondson SD, Zhu C, ((Kar N-F)), Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, ((Shen D-M)), 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 | title = Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.| journal = Journal of Medicinal Chemistry | volume = 59 | issue = 2 | pages = 609-23 | date = January 2016 | pmid = 26709102 | doi = 10.1021/acs.jmedchem.5b01372 }}</ref>


==Antagonists==
=== Antagonists ===
''([[Beta blocker]]s)''<ref name="pmid8569714">{{cite journal | author = Nisoli E, Tonello C, Landi M, Carruba MO | title = Functional studies of the first selective β<sub>3</sub>-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 = }}</ref>


==See also==
* L-748,328<ref name="pmid10411574" />
*Other [[adrenergic receptors]]
* L-748,337<ref name="pmid10411574" />
* [[SR 59230A]] was thought to be a selective β<sub>3</sub> [[Receptor antagonist|antagonist]]<ref name="pmid8569714">{{cite journal | vauthors = Nisoli E, Tonello C, Landi M, Carruba MO | title = Functional studies of the first selective β<sub>3</sub>-adrenergic receptor antagonist SR 59230A in rat brown adipocytes | journal = Mol. Pharmacol. | volume = 49 | issue = 1 | pages = 7–14 | year = 1996 | pmid = 8569714 | doi =  }}</ref> but later found to also be an antagonist of the α<sub>1</sub> receptor.<ref name="pmid19422394">{{cite journal | vauthors = Bexis S, Docherty JR | title = Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse | journal = British Journal of Pharmacology | volume = 158 | issue = 1 | pages = 259–66 | date = April 2009 | pmid = 19422394 | pmc = 2795232 | doi = 10.1111/j.1476-5381.2009.00186.x }}</ref>
 
== Interactions ==
 
Beta-3 adrenergic receptor has been shown to [[Protein-protein interaction|interact]] with [[Src (gene)|Src]].<ref name="pmid11013230">{{cite journal | vauthors = Cao W, Luttrell LM, Medvedev AV, Pierce KL, Daniel KW, Dixon TM, Lefkowitz RJ, Collins S | 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 = 2000 | pmid = 11013230 | doi = 10.1074/jbc.C000592200 }}</ref>
 
== See also ==
*Other [[adrenergic receptor]]s
**[[Alpha-1 adrenergic receptor]]
**[[Alpha-1 adrenergic receptor]]
**[[Alpha-2 adrenergic receptor]]
**[[Alpha-2 adrenergic receptor]]
**[[Beta-1 adrenergic receptor]]  
**[[Beta-1 adrenergic receptor]]
**[[Beta-2 adrenergic receptor]]  
**[[Beta-2 adrenergic receptor]]
**[[Beta Blocker]]
 
== References ==
{{Reflist|35em}}
 
== Further reading ==
{{Refbegin|35em}}
* {{cite journal | vauthors = 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 | vauthors = Nahmias C, Blin N, Elalouf JM, Mattei MG, Strosberg AD, Emorine LJ | 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 | pmc = 453106 | doi =  }}
* {{cite journal | vauthors = Emorine LJ, Marullo S, Briend-Sutren MM, Patey G, Tate K, Delavier-Klutchko C, Strosberg AD | title = Molecular characterization of the human beta 3-adrenergic receptor | journal = Science | volume = 245 | issue = 4922 | pages = 1118–21 | year = 1989 | pmid = 2570461 | doi = 10.1126/science.2570461 }}
* {{cite journal | vauthors = 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 | vauthors = Rodriguez M, Carillon C, Coquerel A, Le Fur G, Ferrara P, Caput D, Shire D | 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 = 10.1016/0169-328X(94)00274-I }}
* {{cite journal | vauthors = Clément K, Vaisse C, Manning BS, Basdevant A, Guy-Grand B, Ruiz J, Silver KD, Shuldiner AR, Froguel P, Strosberg AD | 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 = 10.1056/NEJM199508103330605 }}
* {{cite journal | vauthors = Dib A, Adélaïde J, Chaffanet M, Imbert A, Le Paslier D, Jacquemier J, Gaudray P, Theillet C, Birnbaum D, Pébusque MJ | 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 | vauthors = 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 = 10.1016/0263-7855(94)80004-9 }}
* {{cite journal | vauthors = Wilkie TM, Chen Y, Gilbert DJ, Moore KJ, Yu L, Simon MI, Copeland NG, Jenkins NA | 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 | vauthors = Krief S, Lönnqvist F, Raimbault S, Baude B, Van Spronsen A, Arner P, Strosberg AD, Ricquier D, Emorine LJ | 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 | pmc = 330032 | doi = 10.1172/JCI116191 }}
* {{cite journal | vauthors = van Spronsen A, Nahmias C, Krief S, Briend-Sutren MM, Strosberg AD, Emorine LJ | 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 = 10.1111/j.1432-1033.1993.tb17861.x }}
* {{cite journal | vauthors = Lelias JM, Kaghad M, Rodriguez M, Chalon P, Bonnin J, Dupre I, Delpech B, Bensaid M, LeFur G, Ferrara P | 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 = 10.1016/0014-5793(93)81377-C }}
* {{cite journal | vauthors = Candelore MR, Deng L, Tota LM, Kelly LJ, Cascieri MA, Strader CD | 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 = 10.1210/en.137.6.2638 }}
* {{cite journal | vauthors = Fujisawa T, Ikegami H, Yamato E, Takekawa K, Nakagawa Y, Hamada Y, Oga T, Ueda H, Shintani M, Fukuda M, Ogihara T | 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 = 10.1007/BF00418352 }}
* {{cite journal | vauthors = Higashi K, Ishikawa T, Ito T, Yonemura A, Shige H, Nakamura H | 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 | vauthors = Hoffstedt J, Poirier O, Thörne A, Lönnqvist F, Herrmann SM, Cambien F, Arner P | 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 = 10.2337/diabetes.48.1.203 }}
* {{cite journal | vauthors = Halushka MK, Fan JB, Bentley K, Hsie L, Shen N, Weder A, Cooper R, Lipshutz R, Chakravarti A | 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 | vauthors = Kimura K, Sasaki N, Asano A, Mizukami J, Kayahashi S, Kawada T, Fushiki T, Morimatsu M, Yoshida T, Saito M | 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 = 10.1055/s-2007-978597 }}
* {{cite journal | vauthors = Cao W, Luttrell LM, Medvedev AV, Pierce KL, Daniel KW, Dixon TM, Lefkowitz RJ, Collins S | 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 | vauthors = Russell ST, Hirai K, Tisdale MJ | title = Role of β3-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 | pmc = 2375201 | doi = 10.1038/sj.bjc.6600086 }}
{{Refend}}


==References==
== External links ==
{{reflist|2}}
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2191 | title = &beta;<sub>3</sub>-adrenoceptor  | accessdate = | authorlink = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | archiveurl = | archivedate = | quote = }}
* {{UCSC gene info|ADRB3}}


==Further reading==
{{G protein-coupled receptors|g1}}
{{refbegin|2}}
{{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 }}
}}
{{refend}}


{{G protein-coupled receptors}}
{{Use dmy dates|date=January 2012}}
[[Category:Adrenergic receptors‎]]
[[Category:G protein coupled receptors]]


{{WH}}
[[Category:Adrenergic receptors]]
{{WS}}

Revision as of 07:18, 1 November 2017

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Identifiers
Aliases
External IDsGeneCards: [1]
Orthologs
SpeciesHumanMouse
Entrez

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Ensembl

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UniProt

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RefSeq (mRNA)

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View/Edit Human

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

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 antistress 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 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

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

Agonists

Antagonists

Interactions

Beta-3 adrenergic receptor has been shown to interact with Src.[15]

See also

References

  1. ↑ 1.0 1.1 "Entrez Gene: ADRB3 adrenergic, beta-3-, receptor".
  2. ↑ 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. ↑ 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. ↑ 8.0 8.1 8.2 Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y, Newbold R, Cascieri MA, Weber AE (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, 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.
  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, 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.
  12. ↑ Edmondson SD, Zhu C, Kar N-F, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen D-M, 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.
  13. ↑ 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.
  14. ↑ 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.
  15. ↑ 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

  • 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, Strosberg AD (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, Shire D (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, Silver KD, Shuldiner AR, Froguel P, Strosberg AD (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, Imbert A, Le Paslier D, Jacquemier J, Gaudray P, Theillet C, Birnbaum D, Pébusque MJ (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, Moore KJ, Yu L, Simon MI, Copeland NG, Jenkins NA (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, Strosberg AD, Ricquier D, Emorine LJ (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.
  • 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, Delpech B, Bensaid M, LeFur G, Ferrara P (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, Oga T, Ueda H, Shintani M, Fukuda M, Ogihara T (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, Arner P (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, Hsie L, Shen N, Weder A, Cooper R, Lipshutz R, Chakravarti A (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, Fushiki T, Morimatsu M, Yoshida T, Saito M (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, Lefkowitz RJ, Collins S (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

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