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 [ICD10: J45]
Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45]
Angina pectoris [ICD9: 413; ICD10: I20]
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.
Ref 522437ClinicalTrials.gov (NCT00753168) Phase 1-2 Evaluation of OT-730 Eye Drops in Reducing the Intraocular Pressure in Patients With Ocular Hypertension or Open-Angle Glaucoma. U.S. National Institutes ofHealth.
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.
Ref 525938Effects of the two beta3-agonists, ZD7114 and ZD2079 on 24 hour energy expenditure and respiratory quotient in obese subjects. Int J Obes Relat Metab Disord. 2000 Dec;24(12):1553-60.
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.
Ref 540400(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: 3462).
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).
Ref 544571Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000171)
Ref 544638Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000393)
Ref 544649Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000427)
Ref 544945Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001618)
Ref 545156Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002312)
Ref 545184Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002399)
Ref 545495Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003470)
Ref 545496Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003472)
Ref 545594Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003832)
Ref 545911Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005323)
Ref 546206Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006890)
Ref 546455Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008218)
Ref 546562Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008959)
Ref 546580Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009043)
Ref 546607Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009164)
Ref 546852Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010623)
Ref 547021Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012159)
Ref 547126Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013231)
Ref 547143Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013384)
Ref 547180Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013676)
Ref 547408Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015988)
Ref 547795Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019361)
Ref 548176Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022773)
Ref 549077Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031995)
Ref 549821Clinical pipeline report, company report or official report of Sanofi-Synthelabo.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525440LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors. Eur J Pharmacol. 1999 Feb 19;367(2-3):431-5.
Ref 525542Potent and selective human beta(3)-adrenergic receptor antagonists. J Pharmacol Exp Ther. 1999 Aug;290(2):649-55.
Ref 525620Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. Mol Pharmacol. 1999 Nov;56(5):875-85.
Ref 525848Comparison of the beta2-adrenoceptor selectivity of rimiterol, salbutamol and isoprenaline by the intravenous route in man. Br J Clin Pharmacol. 1975 Feb;2(1):41-8.
Ref 526315Mouse beta 3a- and beta 3b-adrenoceptors expressed in Chinese hamster ovary cells display identical pharmacology but utilize distinct signalling pathways. Br J Pharmacol. 2002 Apr;135(8):1903-14.
Ref 526702Pharmacological profile of KUL-7211, a selective beta-adrenoceptor agonist, in isolated ureteral smooth muscle. J Pharmacol Sci. 2003 Aug;92(4):411-9.
Ref 526944Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors. Eur J Pharmacol. 2004 Jan 26;484(2-3):323-31.
Ref 527007Markedly reduced effects of (-)-isoprenaline but not of (-)-CGP12177 and unchanged affinity of beta-blockers at Gly389-beta1-adrenoceptors compared to Arg389-beta1-adrenoceptors. Br J Pharmacol. 2004May;142(1):51-6. Epub 2004 Mar 22.
Ref 527025Binding of (-)-[3H]-CGP12177 at two sites in recombinant human beta 1-adrenoceptors and interaction with beta-blockers. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):525-32. Epub 2004 Apr 2.
Ref 527168Pharmacological characterization of beta-adrenoceptor subtypes mediating relaxation in porcine isolated ureteral smooth muscle. J Urol. 2004 Sep;172(3):1155-9.
Ref 528534Lack of an effect of a novel beta3-adrenoceptor agonist, TAK-677, on energy metabolism in obese individuals: a double-blind, placebo-controlled randomized study. J Clin Endocrinol Metab. 2007 Feb;92(2):527-31. Epub 2006 Nov 21.
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.
Ref 530320Pharmacokinetics of epanolol after acute and chronic oral dosing in elderly patients with stable angina pectoris. Br J Clin Pharmacol. 1990 Mar;29(3):333-7.
Ref 530883Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands.
Ref 530999The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. Br J Pharmacol. 2010 Jul;160(5):1048-61.
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).
Ref 544004Pindolol--a beta-adrenoceptor blocking drug with partial agonist activity: clinical pharmacological considerations.. Br J Clin Pharmacol. 1982; 13(Suppl 2): 187S-192S.
Ref 544405Combination of a Beta Adrenoceptor Modulator and a Norepinephrine-Serotonin Uptake Inhibitor for the Treatment of Obesity. ACS Med Chem Lett. 2011 August 11; 2(8): 583-586.
Ref 548857Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029610)
Ref 549065Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031896)
Ref 549748PW 2101 Penwest discontinued, USA (hypertension) Penwest non-approvable, USA (hypertension), R & D Focus Drug News. July 11, 2005
Ref 549952A Nitric Oxide-Releasing Salbutamol Elicits Potent Relaxant and Anti-Inflammatory Activities. JPET July 2004 vol. 310 no. 1 367-375.
Ref 550845CA patent application no. 630818, Pharmaceutical composition for prevention or treatment of neurogenic pain.
Ref 550931US patent application no. 9,062,094, Dipeptide-based prodrug linkers for aliphatic amine-containing drugs.
Ref 551185News and Analysis. Nature Reviews Drug Discovery 1, 257-258 (April 2002).
Ref 551556Clinical pipeline report, company report or official report of QLT Inc.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551898CA patent application no. 509835, Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof.
Ref 551914CN patent application no. 1717230, Pharmaceutical composition comprising a beta-3-adrenoceptor agonist and a serotonin and/or norepinephrine reuptake inhibitor.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.