Target Information

Target General Information

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Target ID

T52522 (Former ID: TTDS00037)

Target Name

Adrenergic receptor beta-2 (ADRB2)

Synonyms

Beta-2 adrenoreceptor; Beta-2 adrenoceptor; Beta-2 adrenergic receptor; B2AR; ADRB2R

Gene Name

ADRB2

Target Type

Successful target

[1]

Disease

[+] 5 Target-related Diseases

Asthma [ICD-11: CA23]

Chronic obstructive pulmonary disease [ICD-11: CA22]

Conduction disorder [ICD-11: BC63]

Preterm labour/delivery [ICD-11: JB00]

Sleep-related breathing disorder [ICD-11: 7A4Z]

Function

The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins.

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BioChemical Class

GPCR rhodopsin

UniProt ID

ADRB2_HUMAN

Sequence

MGQPGNGSAFLLAPNGSHAPDHDVTQERDEVWVVGMGIVMSLIVLAIVFGNVLVITAIAK
FERLQTVTNYFITSLACADLVMGLAVVPFGAAHILMKMWTFGNFWCEFWTSIDVLCVTAS
IETLCVIAVDRYFAITSPFKYQSLLTKNKARVIILMVWIVSGLTSFLPIQMHWYRATHQE
AINCYANETCCDFFTNQAYAIASSIVSFYVPLVIMVFVYSRVFQEAKRQLQKIDKSEGRF
HVQNLSQVEQDGRTGHGLRRSSKFCLKEHKALKTLGIIMGTFTLCWLPFFIVNIVHVIQD
NLIRKEVYILLNWIGYVNSGFNPLIYCRSPDFRIAFQELLCLRRSSLKAYGNGYSSNGNT
GEQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSQGRNCSTNDSLL

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3D Structure

Click to Show 3D Structure of This Target

PDB

ADReCS ID

BADD_A02053 ; BADD_A04210 ; BADD_A06316

HIT2.0 ID

T92UWJ

Drugs and Modes of Action

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Approved Drug(s)

[+] 19 Approved Drugs

Arformoterol

Drug Info

Approved

Chronic obstructive pulmonary disease

[2], [3]

Bambuterol

Drug Info

Approved

Asthma

[4], [5]

Clenbuterol

Drug Info

Approved

Chronic breathing disorder

[6]

Fenoterol

Drug Info

Approved

Asthma

[7], [8]

Formoterol

Drug Info

Approved

Asthma

[9], [10]

GW642444

Drug Info

Approved

Asthma

[11], [12]

Indacaterol

Drug Info

Approved

Chronic obstructive pulmonary disease

[13], [14]

Isoetharine

Drug Info

Approved

Asthma

[15], [16]

Isoproterenol

Drug Info

Approved

Heart block

[17]

Levalbuterol

Drug Info

Approved

Asthma

[18], [19]

Metaproterenol Sulfate

Drug Info

Approved

Asthma

[18], [20], [21]

Olodaterol

Drug Info

Approved

Chronic obstructive pulmonary disease

[22], [23]

Pirbuterol

Drug Info

Approved

Asthma

[24], [5]

Procaterol

Drug Info

Approved

Asthma

[25], [26]

Ritodrine

Drug Info

Approved

Premature labour

[27], [28]

Salbutamol

Drug Info

Approved

Acute asthma

[29], [30]

Salmeterol

Drug Info

Approved

Chronic obstructive pulmonary disease

[31], [5]

Terbutaline

Drug Info

Approved

Asthma

[32], [33]

Vilanterol

Drug Info

Approved

Chronic obstructive pulmonary disease

[18], [34], [35]

Clinical Trial Drug(s)

[+] 17 Clinical Trial Drugs

GSK642444

Drug Info

Phase 3

Chronic obstructive pulmonary disease

[36]

ICI 118,551

Drug Info

Phase 3

Gastric adenocarcinoma

[37]

PT005

Drug Info

Phase 3

Chronic obstructive pulmonary disease

[38]

QVA-149

Drug Info

Phase 3

Chronic obstructive pulmonary disease

[39]

BUCINDOLOL

Drug Info

Phase 2/3

Atrial fibrillation

[40]

APD-209

Drug Info

Phase 2

Cachexia

[41]

AZD-2115

Drug Info

Phase 2

Chronic obstructive pulmonary disease

[42]

AZD-3199

Drug Info

Phase 2

Asthma

[43]

Carmoterol

Drug Info

Phase 2

Chronic obstructive pulmonary disease

[44], [36]

GSK961081

Drug Info

Phase 2

Chronic obstructive pulmonary disease

[45]

LAS 100977

Drug Info

Phase 2

Chronic obstructive pulmonary disease

[46]

MN-221

Drug Info

Phase 2

Exacerbation of acute asthma

[47]

R-salbutamol sulphate

Drug Info

Phase 2

Skin infection

[48]

TA-2005

Drug Info

Phase 2

Chronic obstructive pulmonary disease

[3]

THRX-198321

Drug Info

Phase 2

Chronic obstructive pulmonary disease

[49]

KUL-7211

Drug Info

Phase 1

Neurogenic bladder dysfunction

[50]

L-796568

Drug Info

Phase 1

Obesity

[51]

Discontinued Drug(s)

[+] 12 Discontinued Drugs

Meluadrine

Drug Info

Discontinued in Preregistration

Premature ejaculation

[52]

Broxaterol

Drug Info

Discontinued in Phase 3

Asthma

[53]

Sibenadet

Drug Info

Discontinued in Phase 3

Chronic obstructive pulmonary disease

[54]

GSK-159797

Drug Info

Discontinued in Phase 2

Chronic obstructive pulmonary disease

[3]

GSK159802

Drug Info

Discontinued in Phase 2

Asthma

[55]

Milveterol

Drug Info

Discontinued in Phase 2

Asthma

[36]

Milveterol+Fluticasone

Drug Info

Discontinued in Phase 2

Chronic obstructive pulmonary disease

[56]

PF-610355

Drug Info

Discontinued in Phase 2

Chronic obstructive pulmonary disease

[57]

Picumeterol

Drug Info

Discontinued in Phase 2

Asthma

[58]

AR-C-89855

Drug Info

Terminated

Chronic obstructive pulmonary disease

[59]

DPI-201-106

Drug Info

Terminated

Cardiovascular disease

[60]

RP-58802B

Drug Info

Terminated

Asthma

[61]

Mode of Action

[+] 4 Modes of Action

Agonist

[+] 31 Agonist drugs

Arformoterol

Drug Info

[62], [63]

Bambuterol

Drug Info

[64]

Clenbuterol

Drug Info

[65], [66]

Fenoterol

Drug Info

[67], [68]

Formoterol

Drug Info

[69], [70], [71]

GW642444

Drug Info

[72]

Indacaterol

Drug Info

[36], [3]

Pirbuterol

Drug Info

[77], [78]

Procaterol

Drug Info

[79], [80]

Salbutamol

Drug Info

[81]

Salmeterol

Drug Info

[82]

Terbutaline

Drug Info

[1]

GSK642444

Drug Info

[11], [12], [36]

PT005

Drug Info

[84]

QVA-149

Drug Info

[36]

APD-209

Drug Info

[88]

AZD-2115

Drug Info

[89]

AZD-3199

Drug Info

[90]

Carmoterol

Drug Info

[36]

LAS 100977

Drug Info

[92]

MN-221

Drug Info

[93]

R-salbutamol sulphate

Drug Info

[94]

TA-2005

Drug Info

[3]

GSK-159797

Drug Info

[3]

GSK159802

Drug Info

[72]

Milveterol

Drug Info

[72]

Milveterol+Fluticasone

Drug Info

[36]

PF-610355

Drug Info

[102]

Picumeterol

Drug Info

[103]

AR-C-89855

Drug Info

[104]

D 2343

Drug Info

[112]

Modulator

[+] 14 Modulator drugs

Isoetharine

Drug Info

[73]

Isoproterenol

Drug Info

[74], [73]

Metaproterenol Sulfate

Drug Info

[76], [73]

Olodaterol

Drug Info

[23]

Ritodrine

Drug Info

[73]

Vilanterol

Drug Info

[34]

BUCINDOLOL

Drug Info

[85], [86], [87]

GSK961081

Drug Info

[91]

THRX-198321

Drug Info

[95]

KUL-7211

Drug Info

[96], [97]

Meluadrine

Drug Info

[99]

Broxaterol

Drug Info

[100]

Sibenadet

Drug Info

[101]

RP-58802B

Drug Info

[107]

Antagonist

[+] 3 Antagonist drugs

Levalbuterol

Drug Info

[75]

ICI 118,551

Drug Info

[83]

Butoxamine

Drug Info

[111]

Inhibitor

[+] 12 Inhibitor drugs

L-796568

Drug Info

[98]

DPI-201-106

Drug Info

[105]

L-755507

Drug Info

[106]

(R,R)-(-)-fenoterol

Drug Info

[108]

(R,S)-(-)-fenoterol

Drug Info

[108]

(S,R)-(+)-fenoterol

Drug Info

[108]

1-(2-allylphenoxy)-3-morpholinopropan-2-ol

Drug Info

[109]

1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol

Drug Info

[109]

2-fluoronorepinehprine

Drug Info

[110]

Dichloroisoproterenol

Drug Info

[113]

GNF-PF-1694

Drug Info

[105]

[3H]CGP12177

Drug Info

[106]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

Top

Target-interacting Proteins

Target-interacting Proteins Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 7 KEGG Pathways

Calcium signaling pathway

cGMP-PKG signaling pathway

cAMP signaling pathway

Neuroactive ligand-receptor interaction

Endocytosis

Adrenergic signaling in cardiomyocytes

Salivary secretion

NetPath Pathway

[+] 1 NetPath Pathways

TCR Signaling Pathway

Panther Pathway

[+] 2 Panther Pathways

Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway

Beta2 adrenergic receptor signaling pathway

PID Pathway

[+] 2 PID Pathways

Arf6 trafficking events

Arf6 signaling events

Reactome

[+] 2 Reactome Pathways

Adrenoceptors

G alpha (s) signalling events

WikiPathways

[+] 7 WikiPathways

Monoamine GPCRs

Calcium Regulation in the Cardiac Cell

GPCRs, Class A Rhodopsin-like

Vitamin D Receptor Pathway

GPCR ligand binding

GPCR downstream signaling

GPCRs, Other

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

Top

REF 1

Evaluation of a new oral beta2-adrenoceptor stimulant bronchodilator, terbutaline. Pharmacology. 1975;13(3):201-11.

REF 2

URL: 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: 7479).

REF 3

Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.

REF 4

REF 5

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 6

Drug information of Clenbuterol, 2008. eduDrugs.

REF 7

REF 8

Acute clenbuterol overdose resulting in supraventricular tachycardia and atrial fibrillation. J Med Toxicol. 2007 Jun;3(2):56-60.

REF 9

REF 10

Long duration of airway but not systemic effects of inhaled formoterol in asthmatic patients. Respir Med. 2008 Mar;102(3):449-56.

REF 11

Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.

REF 12

Vilanterol trifenatate, a novel inhaled long-acting beta2 adrenoceptor agonist, is well tolerated in healthy subjects and demonstrates prolonged bronchodilation in subjects with asthma and COPD. PulmPharmacol Ther. 2013 Apr;26(2):256-64.

REF 13

REF 14

2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.

REF 15

REF 16

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 086711.

REF 17

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083346.

REF 18

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 19

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005434)

REF 20

REF 21

Drug information of Orciprenaline, 2008. eduDrugs.

REF 22

REF 23

2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.

REF 24

REF 25

REF 26

Drug information of Procaterol, 2008. eduDrugs.

REF 27

REF 28

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071438.

REF 29

REF 30

Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.

REF 31

REF 32

REF 33

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075877.

REF 34

REF 35

ClinicalTrials.gov (NCT01936649) Open-label, Test-retest Study Assessing Reproducibility of Quantitative Measurements of Myocardial Uptake of AdreView.. U.S. National Institutes of Health.

REF 36

Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94.

REF 37

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 38

ClinicalTrials.gov (NCT02343458) Study to Assess the Efficacy and Safety of PT003, PT005, and PT001 in Subjects With Moderate to Very Severe COPD. U.S. National Institutes of Health.

REF 39

Clinical pipeline report, company report or official report of Novartis.

REF 40

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 41

ClinicalTrials.gov (NCT01977443) Therapeutic Efficacy of APD-209 Eye Drops in Treatment of Epidemic Keratoconjunctivitis (EKC). U.S. National Institutes of Health.

REF 42

ClinicalTrials.gov (NCT02109406) Efficacy and Safety Study of Two Dose Levels of AZD2115 in Subjects With Moderate to Severe COPD. U.S. National Institutes of Health.

REF 43

ClinicalTrials.gov (NCT00736489) Single-dose Crossover Study to Investigate Pharmacodynamics of AZD3199. U.S. National Institutes of Health.

REF 44

REF 45

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024247)

REF 46

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026746)

REF 47

ClinicalTrials.gov (NCT00683449) Study Evaluating the Safety and Effects of MN-221 in Subjects Experiencing an Acute Exacerbation of Asthma. U.S. National Institutes of Health.

REF 48

ClinicalTrials.gov (NCT00625521) Efficacy and Safety of ASF-1096 Cream 0.5% in the Treatment of Discoid Lupus Erythematosus (DLE) Lesions. U.S. National Institutes of Health.

REF 49

Clinical pipeline report, company report or official report of Theravance.

REF 50

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013676)

REF 51

Effect of a 28-d treatment with L-796568, a novel beta(3)-adrenergic receptor agonist, on energy expenditure and body composition in obese men. Am J Clin Nutr. 2002 Oct;76(4):780-8.

REF 52

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003111)

REF 53

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000105)

REF 54

Anti-obesity drugs and neural circuits of feeding. Trends Pharmacol Sci. 2008 Apr;29(4):208-17.

REF 55

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021784)

REF 56

Clinical pipeline report, company report or official report of GlaxoSmithKline.

REF 57

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025582)

REF 58

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002942)

REF 59

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013263)

REF 60

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000134)

REF 61

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001694)

REF 62

Arformoterol tartrate in the treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease. Drugs Today (Barc). 2009 Jan;45(1):3-9.

REF 63

Arformoterol: (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.

REF 64

Enantiomeric separation of beta2-agonists on macrocyclic antibiotic chiral stationary phases in high performance liquid chromatography. Pharmazie. 2007 Nov;62(11):836-40.

REF 65

Postischemic brain injury is attenuated in mice lacking the beta2-adrenergic receptor. Anesth Analg. 2009 Jan;108(1):280-7.

REF 66

Beta(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.

REF 67

Functional alpha1- and beta2-adrenergic receptors in human osteoblasts. J Cell Physiol. 2009 Jul;220(1):267-75.

REF 68

Effect 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.

REF 69

Long-acting beta2-agonists for chronic obstructive pulmonary disease patients with poorly reversible airflow limitation. Cochrane Database Syst Rev. 2002;(3):CD001104.

REF 70

Tocolytic effects of a long-acting beta2-adrenoceptor agonist, formoterol, in rats. J Pharm Pharmacol. 2000 Nov;52(11):1417-23.

REF 71

Long-acting beta2-agonists for chronic obstructive pulmonary disease. Cochrane Database Syst Rev. 2000;(2):CD001104.

REF 72

Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).

REF 73

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 74

Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404.

REF 75

Beta-blockers in the treatment of hypertension: are there clinically relevant differences Postgrad Med. 2009 May;121(3):90-8.

REF 76

Male--female differences in the impact of beta-adrenoceptor stimulation on resistance to experimental metastasis: exploring the effects of age and ... J Neuroimmunol. 2008 Jan;193(1-2):113-9.

REF 77

Inhaled beta agonists. Respir Care. 2007 Jul;52(7):820-32.

REF 78

A chemical biology approach identifies a beta-2 adrenergic receptor agonist that causes human tumor regression by blocking the Raf-1/Mek-1/Erk1/2 p... Oncogene. 2007 May 31;26(26):3777-88.

REF 79

Inhalation and incubation with procaterol increases diaphragm muscle contractility in mice. Allergol Int. 2007 Sep;56(3):285-91.

REF 80

beta 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.

REF 81

Potential of beta2-adrenoceptor agonists as add-on therapy for multiple sclerosis: focus on salbutamol (albuterol). CNS Drugs. 2002;16(1):1-8.

REF 82

Pharmacogenetic tests in asthma therapy. Clin Lab Med. 2008 Dec;28(4):645-65.

REF 83

Selective beta 2-adrenoceptor antagonists: derivatives of ICI 118,551 and a binary aryloxypropanolamine. J Pharm Pharmacol. 1988 Nov;40(11):803-5.

REF 84

Clinical pipeline report, company report or official report of Pearl Therapeutics.

REF 85

Bucindolol has serotonin and alpha-adrenoceptor blocking properties. J Cardiovasc Pharmacol. 1985;7 Suppl 7:S67-9.

REF 86

Bucindolol, a nonselective beta 1- and beta 2-adrenergic receptor antagonist, decreases beta-adrenergic receptor density in cultured embryonic chic... J Cardiovasc Pharmacol. 2001 Jun;37(6):678-91.

REF 87

Bucindolol: new hopes from reviewing past data.Drugs Today (Barc).2011 May;47(5):347-51.

REF 88

Drugs in development for treatment of patients with cancer-related anorexia and cachexia syndrome. Retraction in: Drug Des Devel Ther. 2013; 7: 1385.

REF 89

Evaluation of WO-2012085582 and WO-2012085583 two identified MABAs: backups to AZD-2115. Expert Opin Ther Pat. 2012 Nov;22(11):1377-83.

REF 90

Clinical pharmacokinetics of AZD3199, an inhaled ultra-long-acting beta2-adrenoreceptor agonist (uLABA). Drug Des Devel Ther. 2015; 9: 753-762.

REF 91

Pharmacologic characterization of GSK-961081 (TD-5959), a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and 2-adrenoceptor agonist properties.J Pharmacol Exp Ther.2014 Oct;351(1):190-9.

REF 92

Pharmacological characterization of abediterol, a novel inhaled beta(2)-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models. J Pharmacol Exp Ther. 2012 Aug;342(2):497-509.

REF 93

Investigation of beta(2)-adrenoceptor subtype selectivity and organ specificity for bedoradrine (KUR-1246), a novel tocolytic beta-adrenergic receptor stimulant. J Obstet Gynaecol Res. 2009 Jun;35(3):405-13.

REF 94

Pharmacokinetics and extrapulmonary beta 2 adrenoceptor activity of nebulised racemic salbutamol and its R and S isomers in healthy volunteers. Thorax. 1997 Oct;52(10):849-52.

REF 95

THRX-198321 is a bifunctional muscarinic receptor antagonist and beta2-adrenoceptor agonist (MABA) that binds in a bimodal and multivalent manner. Mol Pharmacol. 2011 Mar;79(3):389-99.

REF 96

The potency of KUL-7211, a selective ureteral relaxant, in isolated canine ureter: comparison with various spasmolytics.Urol Res.2005 Dec;33(6):409-14.

REF 97

Pharmacological profile of KUL-7211, a selective beta-adrenoceptor agonist, in isolated ureteral smooth muscle. J Pharmacol Sci. 2003 Aug;92(4):411-9.

REF 98

Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic pr... Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9.

REF 99

Effects of meluadrine tartrate and ritodrine hydrochloride on oxytocin-induced uterine contraction, uterine arterial blood flow and maternal cardiovascular function in pregnant goats. Jpn J Pharmacol. 2002 Oct;90(2):107-13.

REF 100

Broxaterol, a new beta 2-adrenoceptor agonist compared to salbutamol in asthmatics, oral and inhalation treatment. Respiration. 1989;55 Suppl 2:15-9.

REF 101

The role of the novel D2/beta2-agonist, Viozan (sibenadet HCl), in the treatment of symptoms of chronic obstructive pulmonary disease: results of a... Respir Med. 2003 Jan;97 Suppl A:S23-33.

REF 102

Inhalation by design: novel ultra-long-acting beta(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup. J Med Chem. 2010 Sep 23;53(18):6640-52.

REF 103

Picumeterol: dissociation of improvement in lung function and reduction of airways hyperresponsiveness in asthmatics. Br J Clin Pharmacol. 1997 Feb;43(2):169-76.

REF 104

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013263)

REF 105

Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5391-5.

REF 106

(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. J Med Chem. 2001 Apr 26;44(9):1456-66.

REF 107

RP 58802B, a long-acting beta 2-adrenoceptor agonist: assessment of antiasthma activity in the guinea-pig in vivo. Pulm Pharmacol. 1992 Sep;5(3):203-12.

REF 108

Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor. J Med Chem. 2007 Jun 14;50(12):2903-15.

REF 109

A vHTS approach for the identification of beta-adrenoceptor ligands. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404.

REF 110

Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines. Bioorg Med Chem. 2009 Dec 1;17(23):7987-92.

REF 111

Partial agonistic effects of carteolol on atypical beta-adrenoceptors in the guinea pig gastric fundus. Jpn J Pharmacol. 2000 Nov;84(3):287-92.

REF 112

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