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 [1]
Bitolterol Drug Info Approved Asthma; Chronic obstructive pulmonary disease [2]
Bopindolol Drug Info Approved Hypertension [2]
Mepindolol Drug Info Approved Angina pectoris [2]
Mirabegron Drug Info Approved Overactive bladder disorder [3], [4]
Nipradilol Drug Info Approved Angina pectoris [2]
Rimiterol Drug Info Approved Asthma [2]
ASP-3652 Drug Info Phase 2 Overactive bladder disorder [5]
AZ-40140 Drug Info Phase 2 Obesity; Type 2 diabetes [6]
CL-316,243 Drug Info Phase 2 Obesity [7], [8]
CP-331684 Drug Info Phase 2 Diabetes [9]
GW-427353 Drug Info Phase 2 Urinary incontinence [10]
LY-362884 Drug Info Phase 2 Obesity; Type 2 diabetes [6]
LY-377604 Drug Info Phase 2 Obesity [11]
MK-4618 Drug Info Phase 2 Overactive bladder disorder [12]
N-5984 Drug Info Phase 2 Obesity; Type 2 diabetes [6]
YM-430 Drug Info Phase 2 Hypertension [13]
ZD2079 Drug Info Phase 2 Diabetes [14]
QLT-091568 Drug Info Phase 1/2 Glaucoma [15]
BMS-196085 Drug Info Phase 1 Diabetes [16]
EPI-12323 combination therapy Drug Info Phase 1 Asthma; Chronic obstructive pulmonary disease [17]
KUC-7483 Drug Info Phase 1 Overactive bladder disorder [18]
KUL-7211 Drug Info Phase 1 Neurogenic bladder dysfunction [19]
Laevo-Bambuterol Drug Info Phase 1 Asthma [20]
ZD7114 Drug Info Phase 1 Diabetes [14]
Amibegron Drug Info Preclinical Major depressive disorder; Obesity; Type 2 diabetes [21], [22]
CL-314698 Drug Info Preclinical Obesity; Type 2 diabetes [6]
CP-114271 Drug Info Preclinical Obesity [6]
GCR-1087 Drug Info Preclinical Obesity; Type 2 diabetes [6]
L-742791 Drug Info Preclinical Obesity [6], [23]
L-751250 Drug Info Preclinical Obesity [6]
Bitolterol Drug Info Withdrawn from market Asthma [2]
Epanolol Drug Info Discontinued in Preregistration Angina pectoris [24]
PW-2101 Drug Info Discontinued in Preregistration Angina pectoris [25]
Amibegron Drug Info Discontinued in Phase 3 Major depressive disorder; Severe mood disorders [21], [22]
Adaprolol maleate-SME Drug Info Discontinued in Phase 2 Glaucoma [26]
ALPRENOXIME HYDROCHLORIDE Drug Info Discontinued in Phase 2 Glaucoma [27]
OBERADILOL MONOETHYL MALEATE Drug Info Discontinued in Phase 2 Hypertension [28]
PROXODOLOL Drug Info Discontinued in Phase 2 Glaucoma [29]
Rafabegron Drug Info Discontinued in Phase 2 Type 2 diabetes [30]
Tienoxolol Drug Info Discontinued in Phase 2 Hypertension [31]
NCX 950 Drug Info Discontinued in Phase 1/2 Asthma [32]
MN-246 Drug Info Discontinued in Phase 1 Urinary incontinence [33]
PAFENOLOL Drug Info Discontinued in Phase 1 Hypertension [34]
RO-16-8714 Drug Info Discontinued in Phase 1 Diabetes [35]
SB 418790 Drug Info Discontinued in Phase 1 Type 2 diabetes [36]
BMS-210285 Drug Info Terminated Type 2 diabetes [37]
BRL 26830A Drug Info Terminated Obesity [38]
BRL 37344 Drug Info Terminated Discovery agent [39], [40]
FR149175 Drug Info Terminated Type 2 diabetes [41]
H-216/44 Drug Info Terminated Glaucoma [42]
SM 11044 Drug Info Terminated Asthma [43]
SR-58878 Drug Info Terminated Irritable bowel syndrome [44]
SR-58894A Drug Info Terminated Gastrointestinal disease [45]
Trecadrine Drug Info Terminated Discovery agent [46]
Agonist (-)-Ro 363 Drug Info [47]
Amibegron Drug Info [21]
ASP-3652 Drug Info [48]
AZ-40140 Drug Info [6]
BMS-210285 Drug Info [49]
BRL 26830A Drug Info [50]
BRL 37344 Drug Info [51]
Carazolol Drug Info [52]
CGP 12177 Drug Info [51]
CL-314698 Drug Info [6]
CL-316,243 Drug Info [53]
CP-114271 Drug Info [6]
CP-331684 Drug Info [54]
EPI-12323 combination therapy Drug Info [55]
FMP-825 Drug Info [56]
FR149175 Drug Info [57]
GCR-1087 Drug Info [6]
GW-427353 Drug Info [6]
KUC-7483 Drug Info [58], [59]
L-742791 Drug Info [6]
L-751250 Drug Info [6]
LY-362884 Drug Info [6]
LY-377604 Drug Info [60]
MK-4618 Drug Info [61]
MN-246 Drug Info [62]
N-5984 Drug Info [6]
NCX 950 Drug Info [63]
prenalterol Drug Info [64]
SB 418790 Drug Info [65]
SB251023 Drug Info [66]
SM 11044 Drug Info [51]
SWR-0342SA Drug Info [67]
T-0509 Drug Info [68]
Trecadrine Drug Info [69]
Trimetoquinol Drug Info [70]
xamoterol Drug Info [71]
ZD2079 Drug Info [72]
ZD7114 Drug Info [72]
zinterol Drug Info [73]
[125I]ICYP Drug Info [74]
[3H](-)CGP 12177 Drug Info [75]
Inhibitor 1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol Drug Info [76]
1-(2-allylphenoxy)-3-morpholinopropan-2-ol Drug Info [77]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol Drug Info [77]
BMS-196085 Drug Info [78]
Modulator Adaprolol maleate-SME Drug Info [79]
ALPRENOXIME HYDROCHLORIDE Drug Info [80]
Amosulalol Drug Info [1], [2]
Bitolterol Drug Info [81], [2]
Bopindolol Drug Info [82], [2]
Epanolol Drug Info [83]
ER-23006 Drug Info [55]
H-216/44 Drug Info [84]
KUL-7211 Drug Info [85]
Laevo-Bambuterol Drug Info [55]
Mepindolol Drug Info [86], [87], [2]
Mirabegron Drug Info [3]
Nipradilol Drug Info [88], [2]
OBERADILOL MONOETHYL MALEATE Drug Info [89]
PAFENOLOL Drug Info [90]
PROXODOLOL Drug Info [91]
Rafabegron Drug Info [92]
Rimiterol Drug Info [93], [2]
RO-16-8714 Drug Info [94]
SR-58878 Drug Info [56]
SR-58894A Drug Info [95]
Tienoxolol Drug Info [96]
YM-430 Drug Info [13]
Binder Beta-adrenoceptor ligands Drug Info [55]
Antagonist cicloprolol Drug Info [97]
H87/07 Drug Info [97]
L-748337 Drug Info [98]
L748328 Drug Info [98]
LK 204-545 Drug Info [97]
NIHP Drug Info [97]
NIP Drug Info [97]
PW-2101 Drug Info [99]
QLT-091568 Drug Info [100]
[125I](-)ICYP Drug Info [101]
Blocker MystiLol Drug Info [55]
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 1Effects 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 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 4(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 5ClinicalTrials.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 6Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
REF 7Effect 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 8(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 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013231)
REF 10ClinicalTrials.gov (NCT00394186) A Study To Investigate GW427353 In Subjects With Irritable Bowel Syndrome (IBS). U.S. National Institutes of Health.
REF 11ClinicalTrials.gov (NCT00993421) A Weight Loss Study in Overweight Men and Women. U.S. National Institutes of Health.
REF 12ClinicalTrials.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 13Cardiovascular 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 14Effects 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 15ClinicalTrials.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 16BMS-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 17Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015988)
REF 18ClinicalTrials.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 19Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013676)
REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031995)
REF 21Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
REF 22(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 23(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 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000427)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019361)
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003472)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003470)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002312)
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009043)
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009164)
REF 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000171)
REF 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012159)
REF 33Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022773)
REF 34Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002399)
REF 35Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001618)
REF 36Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013384)
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010623)
REF 38Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000393)
REF 39(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 40Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006890)
REF 41Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008959)
REF 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005323)
REF 43The iodocyanopindolol and SM-11044 binding protein belongs to the TM9SF multispanning membrane protein superfamily. Gene. 2001 Aug 8;273(2):227-37.
REF 44Clinical pipeline report, company report or official report of Sanofi-Synthelabo.
REF 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008218)
REF 46Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003832)
REF 47Effects 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 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029610)
REF 49CA patent application no. 509835, Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof.
REF 50Anti-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 51Effects 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 52Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404.
REF 53Beta 3-adrenoceptor agonists as anti-diabetic and anti-obesity drugs in humans. Curr Pharm Des. 2001 Sep;7(14):1433-49.
REF 54CN patent application no. 1717230, Pharmaceutical composition comprising a beta-3-adrenoceptor agonist and a serotonin and/or norepinephrine reuptake inhibitor.
REF 55(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 56(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 57FR149175, 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 58Mirabegron for the treatment of overactive bladder. Drugs Today (Barc). 2012 Jan;48(1):25-32.
REF 59Effects 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 60Combination 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 61Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031896)
REF 62CA patent application no. 630818, Pharmaceutical composition for prevention or treatment of neurogenic pain.
REF 63A Nitric Oxide-Releasing Salbutamol Elicits Potent Relaxant and Anti-Inflammatory Activities. JPET July 2004 vol. 310 no. 1 367-375.
REF 64Beta 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 65News and Analysis. Nature Reviews Drug Discovery 1, 257-258 (April 2002).
REF 66Mouse 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 67Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
REF 68Molecular characterization of pharmacological properties of T-0509 for beta-adrenoceptors. Eur J Pharmacol. 1996 Nov 21;315(3):363-7.
REF 69Potential anti-diabetic applications of a new molecule with affinity for beta 3-adrenoceptors. Life Sci. 1996;59(11):PL141-6.
REF 70Synthesis 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 71Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. Mol Pharmacol. 1999 Nov;56(5):875-85.
REF 72Urinary tract toxicity in rats following administration of beta 3-adrenoceptor agonists. Toxicol Pathol. 1999 Mar-Apr;27(2):165-70.
REF 73The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. Br J Pharmacol. 2010 Jul;160(5):1048-61.
REF 74Stereoselectivity 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 75Binding 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 76J 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 77Bioorg 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 78Bioorg 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 79Synthesis and pharmacological activity of adaprolol enantiomers: a new soft drug for treating glaucoma. J Ocul Pharmacol Ther. 1996 Summer;12(2):115-22.
REF 80Improved delivery through biological membranes. LVI. Pharmacological evaluation of alprenoxime--a new potential antiglaucoma agent. Pharm Res. 1991 Nov;8(11):1389-95.
REF 81Bitolterol mesylate: a beta-adrenergic agent. Chemistry, pharmacokinetics, pharmacodynamics, adverse effects and clinical efficacy in asthma. Pharmacotherapy. 1985 May-Jun;5(3):127-37.
REF 82Effect of propranolol, alprenolol, pindolol, and bopindolol on beta 2-adrenoceptor density in human lymphocytes. J Cardiovasc Pharmacol. 1986;8 Suppl 6:S70-3.
REF 83Pharmacokinetics 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 84Binding of the beta-blockers timolol and H 216/44 to ocular melanin. Exp Eye Res. 1988 Oct;47(4):565-77.
REF 85Pharmacological profile of KUL-7211, a selective beta-adrenoceptor agonist, in isolated ureteral smooth muscle. J Pharmacol Sci. 2003 Aug;92(4):411-9.
REF 86Pharmacological studies on the intrinsic sympathomimetic activity of the beta-adrenoceptor antagonist mepindolol. Arzneimittelforschung. 1986 May;36(5):811-3.
REF 87Pindolol--a beta-adrenoceptor blocking drug with partial agonist activity: clinical pharmacological considerations.. Br J Clin Pharmacol. 1982; 13(Suppl 2): 187S-192S.
REF 88Actions 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 89US patent application no. 9,062,094, Dipeptide-based prodrug linkers for aliphatic amine-containing drugs.
REF 90Presystemic 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 91The 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 92Lack 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 93Comparison 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 94The 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 95Pharmacological characterization of beta-adrenoceptor subtypes mediating relaxation in porcine isolated ureteral smooth muscle. J Urol. 2004 Sep;172(3):1155-9.
REF 96Effects 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 97LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors. Eur J Pharmacol. 1999 Feb 19;367(2-3):431-5.
REF 98Potent and selective human beta(3)-adrenergic receptor antagonists. J Pharmacol Exp Ther. 1999 Aug;290(2):649-55.
REF 99PW 2101 Penwest discontinued, USA (hypertension) Penwest non-approvable, USA (hypertension), R & D Focus Drug News. July 11, 2005
REF 100Clinical pipeline report, company report or official report of QLT Inc.
REF 101Markedly 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.

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