Target Information

Target General Infomation
Target ID
T51408
Former ID
TTDC00184
Target Name
Beta-3 adrenergic receptor
Gene Name
ADRB3
Synonyms
Beta-3 adrenoceptor; Beta-3 adrenoreceptor; Beta3-AR; Beta3AR; ADRB3
Target Type
Successful
Disease Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45]
Angina pectoris [ICD9: 413; ICD10: I20]
Asthma [ICD10: J45]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Gastrointestinal disease [ICD10: K00-K93]
Hypertension [ICD9: 401; ICD10: I10-I16]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Major depressive disorder; Severe mood disorders [ICD9: 296, 296.2, 296.3; ICD10: F30-F39, F32, F33]
Major depressive disorder; Obesity; Type 2 diabetes [ICD9: 250, 250.00, 250.02, 278, 296, 296.2, 296.3; ICD10: E08-E13, E11, E66, F30-F39, F32, F33]
Neurogenic bladder dysfunction [ICD10: N31.9]
Obesity; Type 2 diabetes [ICD9: 250, 250.00, 250.02, 278; ICD10: E08-E13, E11, E66]
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Obesity [ICD9: 278; ICD10: E66]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Function
Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis.
BioChemical Class
GPCR rhodopsin
Target Validation
T51408
UniProt ID
P13945
Sequence
MAPWPHENSSLAPWPDLPTLAPNTANTSGLPGVPWEAALAGALLALAVLATVGGNLLVIV
AIAWTPRLQTMTNVFVTSLAAADLVMGLLVVPPAATLALTGHWPLGATGCELWTSVDVLC
VTASIETLCALAVDRYLAVTNPLRYGALVTKRCARTAVVLVWVVSAAVSFAPIMSQWWRV
GADAEAQRCHSNPRCCAFASNMPYVLLSSSVSFYLPLLVMLFVYARVFVVATRQLRLLRG
ELGRFPPEESPPAPSRSLAPAPVGTCAPPEGVPACGRRPARLLPLREHRALCTLGLIMGT
FTLCWLPFFLANVLRALGGPSLVPGPAFLALNWLGYANSAFNPLIYCRSPDFRSAFRRLL
CRCGRRLPPEPCAAARPALFPSGVPAARSSPAQPRLCQRLDGASWGVS
Structure
2LSQ; 2CDW
Drugs and Mode of Action
Drug(s) Amosulalol Drug Info Approved Hypertension [533886]
Bitolterol Drug Info Approved Asthma; Chronic obstructive pulmonary disease [551871]
Bopindolol Drug Info Approved Hypertension [551871]
Mepindolol Drug Info Approved Angina pectoris [551871]
Mirabegron Drug Info Approved Overactive bladder disorder [532210], [542469]
Nipradilol Drug Info Approved Angina pectoris [551871]
Rimiterol Drug Info Approved Asthma [551871]
ASP-3652 Drug Info Phase 2 Overactive bladder disorder [523939]
AZ-40140 Drug Info Phase 2 Obesity; Type 2 diabetes [536122]
CL-316,243 Drug Info Phase 2 Obesity [533802], [540400]
CP-331684 Drug Info Phase 2 Diabetes [547126]
GW-427353 Drug Info Phase 2 Urinary incontinence [521908]
LY-362884 Drug Info Phase 2 Obesity; Type 2 diabetes [536122]
LY-377604 Drug Info Phase 2 Obesity [522816]
MK-4618 Drug Info Phase 2 Overactive bladder disorder [523395]
N-5984 Drug Info Phase 2 Obesity; Type 2 diabetes [536122]
YM-430 Drug Info Phase 2 Hypertension [534350]
ZD2079 Drug Info Phase 2 Diabetes [525938]
QLT-091568 Drug Info Phase 1/2 Glaucoma [522437]
BMS-196085 Drug Info Phase 1 Diabetes [526197]
EPI-12323 combination therapy Drug Info Phase 1 Asthma; Chronic obstructive pulmonary disease [547408]
KUC-7483 Drug Info Phase 1 Overactive bladder disorder [524942]
KUL-7211 Drug Info Phase 1 Neurogenic bladder dysfunction [547180]
Laevo-Bambuterol Drug Info Phase 1 Asthma [549077]
ZD7114 Drug Info Phase 1 Diabetes [525938]
Amibegron Drug Info Preclinical Major depressive disorder; Obesity; Type 2 diabetes [536580], [541023]
CL-314698 Drug Info Preclinical Obesity; Type 2 diabetes [536122]
CP-114271 Drug Info Preclinical Obesity [536122]
GCR-1087 Drug Info Preclinical Obesity; Type 2 diabetes [536122]
L-742791 Drug Info Preclinical Obesity [536122], [540405]
L-751250 Drug Info Preclinical Obesity [536122]
Bitolterol Drug Info Withdrawn from market Asthma [551871]
Epanolol Drug Info Discontinued in Preregistration Angina pectoris [544649]
PW-2101 Drug Info Discontinued in Preregistration Angina pectoris [547795]
Amibegron Drug Info Discontinued in Phase 3 Major depressive disorder; Severe mood disorders [536580], [541023]
Adaprolol maleate-SME Drug Info Discontinued in Phase 2 Glaucoma [545496]
ALPRENOXIME HYDROCHLORIDE Drug Info Discontinued in Phase 2 Glaucoma [545495]
OBERADILOL MONOETHYL MALEATE Drug Info Discontinued in Phase 2 Hypertension [545156]
PROXODOLOL Drug Info Discontinued in Phase 2 Glaucoma [546580]
Rafabegron Drug Info Discontinued in Phase 2 Type 2 diabetes [546607]
Tienoxolol Drug Info Discontinued in Phase 2 Hypertension [544571]
NCX 950 Drug Info Discontinued in Phase 1/2 Asthma [547021]
MN-246 Drug Info Discontinued in Phase 1 Urinary incontinence [548176]
PAFENOLOL Drug Info Discontinued in Phase 1 Hypertension [545184]
RO-16-8714 Drug Info Discontinued in Phase 1 Diabetes [544945]
SB 418790 Drug Info Discontinued in Phase 1 Type 2 diabetes [547143]
BMS-210285 Drug Info Terminated Type 2 diabetes [546852]
BRL 26830A Drug Info Terminated Obesity [544638]
BRL 37344 Drug Info Terminated Discovery agent [541013], [546206]
FR149175 Drug Info Terminated Type 2 diabetes [546562]
H-216/44 Drug Info Terminated Glaucoma [545911]
SM 11044 Drug Info Terminated Asthma [526162]
SR-58878 Drug Info Terminated Irritable bowel syndrome [549821]
SR-58894A Drug Info Terminated Gastrointestinal disease [546455]
Trecadrine Drug Info Terminated Discovery agent [545594]
Agonist (-)-Ro 363 Drug Info [534368]
Amibegron Drug Info [536580]
ASP-3652 Drug Info [548857]
AZ-40140 Drug Info [536122]
BMS-210285 Drug Info [551898]
BRL 26830A Drug Info [536256]
BRL 37344 Drug Info [537970]
Carazolol Drug Info [538095]
CGP 12177 Drug Info [537970]
CL-314698 Drug Info [536122]
CL-316,243 Drug Info [535218]
CP-114271 Drug Info [536122]
CP-331684 Drug Info [551914]
EPI-12323 combination therapy Drug Info [543746]
FMP-825 Drug Info [543754]
FR149175 Drug Info [538035]
GCR-1087 Drug Info [536122]
GW-427353 Drug Info [536122]
KUC-7483 Drug Info [531824], [531877]
L-742791 Drug Info [536122]
L-751250 Drug Info [536122]
LY-362884 Drug Info [536122]
LY-377604 Drug Info [544405]
MK-4618 Drug Info [549065]
MN-246 Drug Info [550845]
N-5984 Drug Info [536122]
NCX 950 Drug Info [549952]
prenalterol Drug Info [533129]
SB 418790 Drug Info [551185]
SB251023 Drug Info [526315]
SM 11044 Drug Info [537970]
SWR-0342SA Drug Info [537068]
T-0509 Drug Info [534301]
Trecadrine Drug Info [537984]
Trimetoquinol Drug Info [534963]
xamoterol Drug Info [525620]
ZD2079 Drug Info [534855]
ZD7114 Drug Info [534855]
zinterol Drug Info [530999]
[125I]ICYP Drug Info [526944]
[3H](-)CGP 12177 Drug Info [527025]
Inhibitor 1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol Drug Info [533374]
1-(2-allylphenoxy)-3-morpholinopropan-2-ol Drug Info [530883]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol Drug Info [530883]
BMS-196085 Drug Info [528868]
Modulator Adaprolol maleate-SME Drug Info [534192]
ALPRENOXIME HYDROCHLORIDE Drug Info [529137]
Amosulalol Drug Info [533886], [551871]
Bitolterol Drug Info [533490], [551871]
Bopindolol Drug Info [532612], [551871]
Epanolol Drug Info [530320]
ER-23006 Drug Info [543746]
H-216/44 Drug Info [533381]
KUL-7211 Drug Info [526702]
Laevo-Bambuterol Drug Info [543746]
Mepindolol Drug Info [533373], [544004], [551871]
Mirabegron Drug Info [532210]
Nipradilol Drug Info [533522], [551871]
OBERADILOL MONOETHYL MALEATE Drug Info [550931]
PAFENOLOL Drug Info [533895]
PROXODOLOL Drug Info [533804]
Rafabegron Drug Info [528534]
Rimiterol Drug Info [525848], [551871]
RO-16-8714 Drug Info [533155]
SR-58878 Drug Info [543754]
SR-58894A Drug Info [527168]
Tienoxolol Drug Info [533973]
YM-430 Drug Info [534350]
Binder Beta-adrenoceptor ligands Drug Info [543746]
Antagonist cicloprolol Drug Info [525440]
H87/07 Drug Info [525440]
L-748337 Drug Info [525542]
L748328 Drug Info [525542]
LK 204-545 Drug Info [525440]
NIHP Drug Info [525440]
NIP Drug Info [525440]
PW-2101 Drug Info [549748]
QLT-091568 Drug Info [551556]
[125I](-)ICYP Drug Info [527007]
Blocker MystiLol Drug Info [543746]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
DRM DRM Info
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
Endocytosis
Salivary secretion
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Beta3 adrenergic receptor signaling pathway
Reactome Adrenoceptors
G alpha (s) signalling events
WikiPathways Monoamine GPCRs
Calcium Regulation in the Cardiac Cell
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 521908ClinicalTrials.gov (NCT00394186) A Study To Investigate GW427353 In Subjects With Irritable Bowel Syndrome (IBS). U.S. National Institutes of Health.
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Ref 522816ClinicalTrials.gov (NCT00993421) A Weight Loss Study in Overweight Men and Women. U.S. National Institutes of Health.
Ref 523395ClinicalTrials.gov (NCT01314872) A Study of the Efficacy and Safety of MK-4618 in Patients With Overactive Bladder (OAB) (MK-4618-008 AM3 EXT1[AM2]). U.S. National Institutes of Health.
Ref 523939ClinicalTrials.gov (NCT01613586) A Randomized Study Comparing Placebo and ASP3652 in the Treatment of Women With Bladder Pain Syndrome / Interstitial Cystitis (BPS/IC). U.S. National Institutes of Health.
Ref 524942ClinicalTrials.gov (NCT02256735) Study to Investigate the Effect of KUC 7483 CL on the QT/QTc Interval of the ECG in Comparison to Placebo and Moxifloxacin in Healthy Male and Female Volunteers. U.S.National Institutes of Health.
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Ref 526162The iodocyanopindolol and SM-11044 binding protein belongs to the TM9SF multispanning membrane protein superfamily. Gene. 2001 Aug 8;273(2):227-37.
Ref 526197BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3041-4.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 533802Effect of CL-316,243, a thermogenic beta 3-agonist, on energy balance and brown and white adipose tissues in rats. Am J Physiol. 1994 Apr;266(4 Pt 2):R1371-82.
Ref 533886Effects of amosulalol, a combined alpha 1- and beta-adrenoceptor-blocking agent, on ischemic myocardial energy metabolism in dogs. J Pharm Sci. 1993 Mar;82(3):291-5.
Ref 534350Cardiovascular effects of YM430, a 1,4-dihydropyridine derivative with beta-adrenoceptor blocking activity, in dogs and rats. Biol Pharm Bull. 1997 Mar;20(3):230-6.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
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Ref 540405(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3467).
Ref 541013(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 567).
Ref 541023(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 568).
Ref 542469(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7445).
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Ref 528868Bioorg Med Chem Lett. 2007 Aug 1;17(15):4290-6. Epub 2007 May 16.Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.
Ref 529137Improved delivery through biological membranes. LVI. Pharmacological evaluation of alprenoxime--a new potential antiglaucoma agent. Pharm Res. 1991 Nov;8(11):1389-95.
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Ref 531824Mirabegron for the treatment of overactive bladder. Drugs Today (Barc). 2012 Jan;48(1):25-32.
Ref 531877Effects of ritobegron (KUC-7483), a novel selective beta3-adrenoceptor agonist, on bladder function in cynomolgus monkey. J Pharmacol Exp Ther. 2012 Jul;342(1):163-8.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 532612Effect of propranolol, alprenolol, pindolol, and bopindolol on beta 2-adrenoceptor density in human lymphocytes. J Cardiovasc Pharmacol. 1986;8 Suppl 6:S70-3.
Ref 533129Beta 1- and beta 2-adrenergic receptor-mediated adenylate cyclase stimulation in nonfailing and failing human ventricular myocardium. Mol Pharmacol. 1989 Mar;35(3):295-303.
Ref 533155The novel thermogenic beta-adrenergic agonist Ro 16-8714 increases the interscapular brown-fat beta-receptor-adenylate cyclase and the uncoupling-protein mRNA level in obese (fa/fa) Zucker rats. Biochem J. 1989 Aug 1;261(3):721-4.
Ref 533373Pharmacological studies on the intrinsic sympathomimetic activity of the beta-adrenoceptor antagonist mepindolol. Arzneimittelforschung. 1986 May;36(5):811-3.
Ref 533374J Med Chem. 1986 Aug;29(8):1524-7.Synthesis and beta-adrenergic receptor blocking potency of 1-(substituted amino)-3-(4-indolyloxy)propan-2-ols.
Ref 533381Binding of the beta-blockers timolol and H 216/44 to ocular melanin. Exp Eye Res. 1988 Oct;47(4):565-77.
Ref 533490Bitolterol mesylate: a beta-adrenergic agent. Chemistry, pharmacokinetics, pharmacodynamics, adverse effects and clinical efficacy in asthma. Pharmacotherapy. 1985 May-Jun;5(3):127-37.
Ref 533522Actions of nipradilol (K-351), a new alpha- and beta-adrenoceptor blocker, on the rabbit portal vein. Jpn J Pharmacol. 1984 Aug;35(4):359-69.
Ref 533804The efficacy of proxodolol, a new beta-adrenoblockader with alpha-adrenoblockader properties, in its single use in patients with stable stenocardia of effort. Eksp Klin Farmakol. 1994 May-Jun;57(3):47-50.
Ref 533886Effects of amosulalol, a combined alpha 1- and beta-adrenoceptor-blocking agent, on ischemic myocardial energy metabolism in dogs. J Pharm Sci. 1993 Mar;82(3):291-5.
Ref 533895Presystemic elimination of the beta-blocker pafenolol in the rat after oral and intraperitoneal administration and identification of a main metabolite in both rats and humans. Drug Metab Dispos. 1993May-Jun;21(3):435-40.
Ref 533973Effects of the beta-adrenoceptor antagonists atenolol and propranolol on human parotid and submandibular-sublingual salivary secretion. J Dent Res. 1994 Jan;73(1):5-10.
Ref 534192Synthesis and pharmacological activity of adaprolol enantiomers: a new soft drug for treating glaucoma. J Ocul Pharmacol Ther. 1996 Summer;12(2):115-22.
Ref 534301Molecular characterization of pharmacological properties of T-0509 for beta-adrenoceptors. Eur J Pharmacol. 1996 Nov 21;315(3):363-7.
Ref 534350Cardiovascular effects of YM430, a 1,4-dihydropyridine derivative with beta-adrenoceptor blocking activity, in dogs and rats. Biol Pharm Bull. 1997 Mar;20(3):230-6.
Ref 534368Effects of (-)-RO363 at human atrial beta-adrenoceptor subtypes, the human cloned beta 3-adrenoceptor and rodent intestinal beta 3-adrenoceptors. Br J Pharmacol. 1997 Jan;120(2):165-76.
Ref 534855Urinary tract toxicity in rats following administration of beta 3-adrenoceptor agonists. Toxicol Pathol. 1999 Mar-Apr;27(2):165-70.
Ref 534963Synthesis and human beta-adrenoceptor activity of 1-(3,5-diiodo-4- methoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-6-ol derivatives in vitro. J Med Chem. 2000 Feb 24;43(4):591-8.
Ref 535218Beta 3-adrenoceptor agonists as anti-diabetic and anti-obesity drugs in humans. Curr Pharm Des. 2001 Sep;7(14):1433-49.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536256Anti-obesity and anti-diabetic actions of a beta 3-adrenoceptor agonist, BRL 26830A, in yellow KK mice. Endocrinol Jpn. 1991 Aug;38(4):397-403.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 537068Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
Ref 537970Effects of several putative beta 3-adrenoceptor agonists on lipolysis in human omental adipocytes. Int J Obes Relat Metab Disord. 1996 May;20(5):428-34.
Ref 537984Potential anti-diabetic applications of a new molecule with affinity for beta 3-adrenoceptors. Life Sci. 1996;59(11):PL141-6.
Ref 538035FR149175, a beta 3-adrenoceptor-selective agonist, is a possible therapeutic agent for non-insulin-dependent diabetes mellitus. Jpn J Pharmacol. 1997 May;74(1):109-12.
Ref 538095Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404.
Ref 543746(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 29).
Ref 543754(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 30).
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