Therapeutic Targets Database
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TTD Target ID: TTDS00037

Target Information
NameBeta-2 adrenergic receptor    
Type of targetSuccessful target    
SynonymsBeta-2 adrenoceptor    
Beta-2 adrenoreceptor    
DiseaseAnxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[1]
Asthma
[ICD9: 493   ICD10: J45]
[2][3][4]
Cardiac arrhythmias
[ICD9: 427   ICD10: I47-I49]
[1]
Chronic obstructive pulmonary disease, unspecified
[ICD9: 460-519, 490-492, 494-496   ICD10: J00-J99, J40-J44, J47]
[5][6]
Depression
[ICD9: 311   ICD10: F32]
[7]
Glaucoma
[ICD9: 365   ICD10: H40-H42]
[8]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[1][9]
Inflammation[2][10]
Multiple sclerosis
[ICD9: 340   ICD10: G35]
[11]
Obstructive airway disease[12]
Respiratory distress syndrome
[ICD9: 518.5, 518.82   ICD10: J80]
[13]
Skeletal muscle wasting[14]
Skeletal muscle weakness
[ICD9: 728.87   ICD10: M62.8]
[14]
Drug(s)ArformoterolApprovedChronic obstructive pulmonary disease[15][16]
BambuterolApprovedAsthma[17]
ClenbuterolApprovedChronic breathing disorders[18][19]
FenoterolApprovedAsthma[20][21]
FormoterolApprovedAsthma[5][22][6]
OrciprenalineApprovedAsthma[23]
PirbuterolApprovedAsthma[24][25]
ProcaterolApprovedAsthma[26][27]
SalbutamolApprovedAcute Asthma[11]
Salbutamol sulphateApprovedAcute Asthma[11]
SalmeterolApprovedChronic obstructive pulmonary disease[28]
Salmeterol xinafoateApprovedAsthma and chronic obstructive pulmonary disease[29][5][30][6][3]
TerbutalineApprovedAsthma[12]
SymbicortCompletedCOPD
SymbicortCompletedSMART
Albuterol sulfatePhase IIIAcute ling injury[31]
Budesonide & formoterol fumarate dihydratePhase IIICOPD & Asthma[32]
GSK642444Phase IIIChronic obstructive pulmonary disease[33]
GW642444Phase IIICOPD & Asthma[34]
IndacaterolPhase IIIChronic obstructive pulmonary disease[33][35]
OlodaterolPhase IIIChronic obstructive pulmonary Disease (COPD)
QVA-149Phase IIIChronic obstructive pulmonary disease[33]
Relvar/BreoPhase IIICOPD mortality outcomes
SymbicortPhase IIIBreath Actuated Inhaler asthma / COPD
VilanterolPhase IIICOPD
CarmoterolPhase II completedChronic obstructive pulmonary disease[33]
GSK961081Phase II completedChronic Obstructive Pulmonary Disease (COPD)[34]
TA-2005Phase II completedChronic obstructive pulmonary disease[35]
961081Phase IICOPD
QMF149Phase IIAsthma, chronic obst ructive pulmonary disease
AnoroSubmittedCOPD
RELVARTM or BREOTM ELLIPTATMFiledCOPD and Asthma
Relvar/BreoSubmittedAsthma
Relvar/BreoSubmittedCOPD
GSK-159797Suspended in Phase II in GSK 2009 ReportChronic obstructive pulmonary disease[35]
GSK159802Suspended in Phase II in GSK 2009 ReportCOPD & Asthma[34]
MilveterolSuspended in Phase II in GSK 2009 ReportCOPD & Asthma[34]
Milveterol+FluticasoneDiscontinued in Phase IIAsthma; Chronic obstructive pulmonary disease[33]
SibenadetDiscontinued in Phase IIIChronic obstructive pulmonary disease[35]
BioChemical ClassTransmembrane protein    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP07550
PDB Structure1GQ4; 2R4R; 2R4S; 2RH1; 3D4S; 3KJ6; 3NY8; 3NY9; 3NYA; 3P0G; 3PDS; 3SN6; 4GBR.    
FunctionBeta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.    
SequenceMGQPGNGSAFLLAPNGSHAPDHDVTQQRDEVWVVGMGIVMSLIVLAIVFGNVLVITAIAK FERLQTVTNYFITSLACADLVMGLAVVPFGAAHILMKMWTFGNFWCEFWTSIDVLCVTAS IETLCVIAVDRYFAITSPFKYQSLLTKNKARVIILMVWIVSGLTSFLPIQMHWYRATHQE AINCYANETCCDFFTNQAYAIASSIVSFYVPLVIMVFVYSRVFQEAKRQLQKIDKSEGRF HVQNLSQVEQDGRTGHGLRRSSKFCLKEHKALKTLGIIMGTFTLCWLPFFIVNIVHVIQD NLIRKEVYILLNWIGYVNSGFNPLIYCRSPDFRIAFQELLCLRRSSLKAYGNGYSSNGNT GEQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSPGRNCSTNDSLL
Related US Patent6,576,793
6,593,497
6,653,323
6,670,376
6,747,043
Target ValidationClick to Find Target Validation Information.    
Inhibitor (R,R)-[36]
(R,S)-[36]
(S,R)-[36]
1- (2-allylphenoxy)-3-morpholinopropan-2-ol[37]
1- (2-isopropylphenoxy)-3-morpholinopropan-2-ol[37]
2-fluoronorepinehprine[38]
BRL-37344[39]
BUCINDOLOL[40]
CGP-12177A[41]
DICHLOROISOPROTERENOL[42]
GNF-PF-1694[43]
ICI-118551[44]
L-755507[41]
L-796568[45]
SDZ-201106[43]
AgonistAlbuterol sulfate[31]
Arformoterol[15][16]
Bambuterol[17]
Budesonide & formoterol fumarate dihydrate[32]
Carmoterol[33]
Clenbuterol[18][19]
D 2343[46]
Fenoterol[20][21]
Formoterol[5][22][6]
GSK-159797[35]
GSK159802[34]
GSK642444[33]
GSK961081[34]
GW642444[34]
Indacaterol[33][35]
Isoprenaline[1]
Metaproterenol[23]
Milveterol[34]
Milveterol+Fluticasone[33]
Orciprenaline[23]
Pirbuterol[24][25]
Procaterol[26][27]
QVA-149[33]
Salbutamol[11]
Salbutamol sulphate[11]
Salmeterol[28]
Salmeterol xinafoate[29][5][30][6][3]
Sibenadet[35]
TA-2005[35]
Terbutaline[12]
AntagonistButoxamine[47]
ICI 118,551[8]
ICI 118.551[48]
Levalbuterol[49]
MultitargetGSK961081[34]
Sibenadet[35]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404. To Reference
Ref 2Pharmacological treatment of asthma today. Eur Respir J Suppl. 2001 Dec;34:34s-40s. To Reference
Ref 3The aliphatic oxidation of salmeterol to alpha-hydroxysalmeterol in human liver microsomes is catalyzed by CYP3A. Drug Metab Dispos. 1996 May;24(5):555-9. To Reference
Ref 4Fenoterol: a beta2-adrenergic agonist for use in asthma. Pharmacology, pharmacokinetics, clinical efficacy and adverse effects. Pharmacotherapy. 1985 May-Jun;5(3):109-26. To Reference
Ref 5Long-acting beta2-agonists for chronic obstructive pulmonary disease patients with poorly reversible airflow limitation. Cochrane Database Syst Rev. 2002;(3):CD001104. To Reference
Ref 6Long-acting beta2-agonists for chronic obstructive pulmonary disease. Cochrane Database Syst Rev. 2000;(2):CD001104. To Reference
Ref 7Neutrophil beta(2)-adrenoceptor function in major depression: G(s) coupling, effects of imipramine and relationship to treatment outcome. Eur J Pharmacol. 1999 Dec 15;386(2-3):135-44. To Reference
Ref 8Selective beta 2-adrenoceptor antagonists: derivatives of ICI 118,551 and a binary aryloxypropanolamine. J Pharm Pharmacol. 1988 Nov;40(11):803-5. To Reference
Ref 9Effect of antihypertensive treatment on the increased beta 2-adrenoceptor density in patients with essential hypertension. Am J Hypertens. 1995 May;8(5 Pt 1):487-93. To Reference
Ref 10The therapeutic potential of long-acting beta 2-adrenoceptor agonists in allergic inflammation. Clin Exp Allergy. 1992 Feb;22(2):177-81. To Reference
Ref 11Potential of beta2-adrenoceptor agonists as add-on therapy for multiple sclerosis: focus on salbutamol (albuterol). CNS Drugs. 2002;16(1):1-8. To Reference
Ref 12Evaluation of a new oral beta2-adrenoceptor stimulant bronchodilator, terbutaline. Pharmacology. 1975;13(3):201-11. To Reference
Ref 13Beta-2-adrenoceptor agonists as inhibitors of lung vascular permeability to radiolabelled transferrin in the adult respiratory distress syndrome in man. Eur J Nucl Med. 1986;12(8):381-4. To Reference
Ref 14Beta 2-agonist fenoterol has greater effects on contractile function of rat skeletal muscles than clenbuterol. Am J Physiol Regul Integr Comp Physiol. 2002 Dec;283(6):R1386-94. Epub 2002 Sep 5. To Reference
Ref 15Arformoterol tartrate in the treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease. Drugs Today (Barc). 2009 Jan;45(1):3-9. To Reference
Ref 16Arformoterol: (R,R)-eformoterol, (R,R)-formoterol, arformoterol tartrate, eformoterol-sepracor, formoterol-sepracor, R,R-eformoterol, R,R-formoterol. Drugs R D. 2004;5(1):25-7. To Reference
Ref 17Enantiomeric separation of beta2-agonists on macrocyclic antibiotic chiral stationary phases in high performance liquid chromatography. Pharmazie. 2007 Nov;62(11):836-40. To Reference
Ref 18Postischemic brain injury is attenuated in mice lacking the beta2-adrenergic receptor. Anesth Analg. 2009 Jan;108(1):280-7. To Reference
Ref 19Beta(2)-adrenoceptor stimulation enhances latent transforming growth factor-beta-binding protein-1 and transforming growth factor-beta1 expression in rat hippocampus after transient forebrain ischemia. Neuroscience. 2001;107(4):593-602. To Reference
Ref 20Functional alpha1- and beta2-adrenergic receptors in human osteoblasts. J Cell Physiol. 2009 Jul;220(1):267-75. To Reference
Ref 21Effect of fenoterol-induced constitutive beta(2)-adrenoceptor activity on contractile receptor function in airway smooth muscle. Eur J Pharmacol. 2001 Nov 23;431(3):353-9. To Reference
Ref 22J Pharm Pharmacol. 2000 Nov;52(11):1417-23.Tocolytic effects of a long-acting beta2-adrenoceptor agonist, formoterol, in rats. To Reference
Ref 23Male--female differences in the impact of beta-adrenoceptor stimulation on resistance to experimental metastasis: exploring the effects of age and gonadal hormone involvement. J Neuroimmunol. 2008 Jan;193(1-2):113-9. Epub 2007 Nov 26. To Reference
Ref 24Inhaled beta agonists. Respir Care. 2007 Jul;52(7):820-32. To Reference
Ref 25A chemical biology approach identifies a beta-2 adrenergic receptor agonist that causes human tumor regression by blocking the Raf-1/Mek-1/Erk1/2 pathway. Oncogene. 2007 May 31;26(26):3777-88. Epub 2007 Jan 29. To Reference
Ref 26Inhalation and incubation with procaterol increases diaphragm muscle contractility in mice. Allergol Int. 2007 Sep;56(3):285-91. Epub 2007 Aug 1. To Reference
Ref 27beta 2-adrenoceptor polymorphism and effect of inhaled beta 2-stimulant (procaterol) on airway resistance measured by body plethysmography in healthy volunteers. Nihon Kokyuki Gakkai Zasshi. 2002 Aug;40(8):637-43. To Reference
Ref 28Pharmacogenetic tests in asthma therapy. Clin Lab Med. 2008 Dec;28(4):645-65. To Reference
Ref 29Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 30Inhaled salmeterol: a review of its efficacy in chronic obstructive pulmonary disease. Drugs Aging. 2001;18(6):441-72. To Reference
Ref 31Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77. To Reference
Ref 32AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 33Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94. To Reference
Ref 34GSK. Product Development Pipeline. February 2009. To Reference
Ref 35Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. To Reference
Ref 36J Med Chem. 2007 Jun 14;50(12):2903-15. Epub 2007 May 17.Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor. To Reference
Ref 37Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands. To Reference
Ref 38Bioorg Med Chem. 2009 Dec 1;17(23):7987-92. Epub 2009 Oct 13.Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines. To Reference
Ref 39J Med Chem. 2003 Jan 2;46(1):105-12.Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence. To Reference
Ref 40J Med Chem. 1980 Mar;23(3):285-9.Antihypertensive indole derivatives of phenoxypropanolamines with beta-adrenergic receptor antagonist and vasodilating activity. To Reference
Ref 41J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. To Reference
Ref 42J Med Chem. 1994 May 13;37(10):1518-25.The [(methyloxy)imino]methyl moiety as a bioisoster of aryl. A novel class of completely aliphatic beta-adrenergic receptor antagonists. To Reference
Ref 43Bioorg Med Chem Lett. 2008 Oct 15;18(20):5391-5. Epub 2008 Sep 14.Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds. To Reference
Ref 44J Med Chem. 2009 Mar 26;52(6):1773-7.Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol. To Reference
Ref 45Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. Epub 2010 Feb 4.Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles. To Reference
Ref 46A new beta 2-adrenoceptor agonist--D 2343--with long duration. Inhalation comparison with terbutaline in asthmatics. Allergy. 1984 Aug;39(6):485-9. To Reference
Ref 47Partial agonistic effects of carteolol on atypical beta-adrenoceptors in the guinea pig gastric fundus. Jpn J Pharmacol. 2000 Nov;84(3):287-92. To Reference
Ref 48Effects of ICI 118.551, a selective beta-2 adrenergic blocking agent on the guinea pig cardiac excitability and ventricular fibrillation threshold. Acta Physiol Hung. 2000;87(1):113-26. To Reference
Ref 49Beta-blockers in the treatment of hypertension: are there clinically relevant differences? Postgrad Med. 2009 May;121(3):90-8. To Reference



 

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Professor in Department of Pharmacy
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