Beta-3 adrenergic receptor

Actions of the β₃ receptor include

• Enhancement of lipolysis in adipose tissue.{{cite journal | vauthors = Ferrer-Lorente R, Cabot C, Fernández-López JA, Alemany M | title = Combined effects of oleoyl-estrone and a β₃-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 | url = https://zenodo.org/record/889563 }}
• Thermogenesis in skeletal muscle{{cite book |author=Rang, H. P. |title=Pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2003 |isbn=0-443-07145-4 }} Page 163

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.{{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 }}

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 G_s.

• Amibegron (SR-58611A){{cite journal | vauthors = Consoli D, Leggio GM, Mazzola C, Micale V, Drago F | title = Behavioral effects of the β₃ 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 }}{{cite journal | vauthors = Overstreet DH, Stemmelin J, Griebel G | title = Confirmation of antidepressant potential of the selective β₃ 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 | s2cid = 35026036 }}
• BRL-37344{{cite journal | vauthors = Mukaida S, Sato M, Öberg AI, Dehvari N, Olsen JM, Kocan M, Halls ML, Merlin J, Sandström AL, Csikasz RI, Evans BA, Summers RJ, Hutchinson DS, Bengtsson T | display-authors = 6 | title = BRL37344 stimulates GLUT4 translocation and glucose uptake in skeletal muscle via β2-adrenoceptors without causing classical receptor desensitization | journal = American Journal of Physiology. Regulatory, Integrative and Comparative Physiology | volume = 316 | issue = 5 | pages = R666–R677 | date = May 2019 | pmid = 30892909 | doi = 10.1152/ajpregu.00285.2018 | doi-access = free }}
• CL-316,243{{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 }}
• L-742,791{{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 }}
• L-796,568{{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 β₃-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 = 10.1093/ajcn/76.4.780| doi-access = free }}
• LY-368,842
• Mirabegron (YM-178),{{cite journal | vauthors = Gras J | title = Mirabegron for the treatment of overactive bladder | journal = Drugs of Today | volume = 48 | issue = 1 | pages = 25–32 | year = 2012 | pmid = 22384458 | doi = 10.1358/dot.2012.48.1.1738056 }} approved for treatment of overactive bladder in Japan, United States, UK, Canada, China and India.
• Nebivolol{{cite journal | vauthors = Rozec B, Erfanian M, Laurent K, Trochu JN, Gauthier C | title = Nebivolol, a vasodilating selective beta(1)-blocker, is a beta(3)-adrenoceptor agonist in the nonfailing transplanted human heart | journal = J Am Coll Cardiol | year = 2009 | volume = 53 | issue = 17 | pages = 1532–8 | doi = 10.1016/j.jacc.2008.11.057 | pmid = 19389564 | doi-access = }} selective beta(1)-blocker and beta(3)-agonist.
• Ro40-2148
• Solabegron (GW-427,353){{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 | s2cid = 19281697 }}
• Vibegron (MK-4618){{cite journal | vauthors = Edmondson SD, Zhu C, Kar NF, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen DM, 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 }}

• L-748,328
• L-748,337
• SR 59230A was thought to be a selective β₃ antagonist{{cite journal | vauthors = 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 }} but later found to also be an antagonist of the α₁ receptor.{{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 }}

Beta-3 adrenergic receptor has been shown to interact with Src.{{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 | doi-access = free }}

• Other adrenergic receptors
• Alpha-1 adrenergic receptor
• Alpha-2 adrenergic receptor
• Beta-1 adrenergic receptor
• Beta-2 adrenergic receptor
• Beta blocker

{{Reflist}}

{{Refbegin|35em}}

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{{Refend}}

• {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2191 | title = β₃-adrenoceptor | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | access-date = 25 November 2008 | archive-date = 30 December 2014 | archive-url = https://web.archive.org/web/20141230175443/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2191 | url-status = dead }}
• {{UCSC gene info|ADRB3}}

{{G protein-coupled receptors|g1}}

Category:Adrenergic receptors