Target General Infomation
Target ID
T52522
Former ID
TTDS00037
Target Name
Beta-2 adrenergic receptor
Gene Name
ADRB2
Synonyms
Beta-2 adrenoceptor; Beta-2 adrenoreceptor; ADRB2
Target Type
Successful
Disease Asthma [ICD10: J45]
Acute asthma [ICD9: 493; ICD10: J45]
Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45]
Asthma; Chronic obstructive pulmonary disease [ICD9:490-492, 494-496; ICD10: J45, J40-J44, J47]
Aging skin; Exacerbations of acute asthma [ICD9:493; ICD10: L00-L99, J45]
Bradycardia; Heart block [ICD9: 116.0, 426.9; ICD10: B40, I44-I45]
Bronchodilator [ICD9: 493; ICD10: J45]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Chronic breathing disorders [ICD9: 490-496; ICD10: J44-J47]
Chronic obstructive pulmonary disease; Asthma [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45]
Cachexia [ICD9: 799.4; ICD10: R64]
Hypertension [ICD9: 401; ICD10: I10-I16]
Neurogenic bladder dysfunction [ICD10: N31.9]
Obesity [ICD9: 278; ICD10: E66]
Premature ejaculation [ICD9: 302.75; ICD10: F52.4]
Premature labour [ICD9: 644, 765; ICD10: O60.1, P07.3]
Skin infections [ICD9: 680-709; ICD10: L00-L99]
Unspecified [ICD code not available]
Function
Beta-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.
BioChemical Class
GPCR rhodopsin
Target Validation
T52522
UniProt ID
Sequence
MGQPGNGSAFLLAPNGSHAPDHDVTQERDEVWVVGMGIVMSLIVLAIVFGNVLVITAIAK
FERLQTVTNYFITSLACADLVMGLAVVPFGAAHILMKMWTFGNFWCEFWTSIDVLCVTAS
IETLCVIAVDRYFAITSPFKYQSLLTKNKARVIILMVWIVSGLTSFLPIQMHWYRATHQE
AINCYANETCCDFFTNQAYAIASSIVSFYVPLVIMVFVYSRVFQEAKRQLQKIDKSEGRF
HVQNLSQVEQDGRTGHGLRRSSKFCLKEHKALKTLGIIMGTFTLCWLPFFIVNIVHVIQD
NLIRKEVYILLNWIGYVNSGFNPLIYCRSPDFRIAFQELLCLRRSSLKAYGNGYSSNGNT
GEQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSQGRNCSTNDSLL
Drugs and Mode of Action
Drug(s) Arformoterol Drug Info Approved Chronic obstructive pulmonary disease [536223], [542501]
Bambuterol Drug Info Approved Asthma [536361], [541721]
Clenbuterol Drug Info Approved Chronic breathing disorders [550744]
Fenoterol Drug Info Approved Asthma [536567], [540946]
Formoterol Drug Info Approved Asthma [536535], [540403]
GW642444 Drug Info Approved Asthma [532150], [532651]
Indacaterol Drug Info Approved Chronic obstructive pulmonary disease [531783], [542479]
Isoetharine Drug Info Approved Asthma [538363], [542219]
Isoproterenol Drug Info Approved Bradycardia; Heart block [538350]
Levalbuterol Drug Info Approved Asthma [545941], [551871]
Metaproterenol Sulfate Drug Info Approved Asthma [551871]
Olodaterol Drug Info Approved Chronic obstructive pulmonary disease [533123], [542545]
Orciprenaline Drug Info Approved Asthma [542268], [550662]
Pirbuterol Drug Info Approved Asthma [536361], [542292]
Procaterol Drug Info Approved Asthma [540402], [550747]
Ritodrine Drug Info Approved Premature labour [538236], [542314]
Salbutamol Drug Info Approved Acute asthma [536500], [540951]
Salmeterol Drug Info Approved Chronic obstructive pulmonary disease [536361], [540957]
Terbutaline Drug Info Approved Asthma [538303], [540968]
Vilanterol Drug Info Approved Asthma; Chronic obstructive pulmonary disease [524423], [542374], [551871]
GSK642444 Drug Info Phase 3 Chronic obstructive pulmonary disease [537130]
PT005 Drug Info Phase 3 Chronic obstructive pulmonary disease [525067]
QVA-149 Drug Info Phase 3 Chronic obstructive pulmonary disease [551966]
APD-209 Drug Info Phase 2 Cachexia [524508]
AZD-2115 Drug Info Phase 2 Chronic obstructive pulmonary disease [524708]
AZD-3199 Drug Info Phase 2 Asthma [522407]
BUCINDOLOL Drug Info Phase 2 Hypertension [524493]
Carmoterol Drug Info Phase 2 Chronic obstructive pulmonary disease [537130], [542572]
GSK961081 Drug Info Phase 2 Chronic obstructive pulmonary disease [548296]
LAS 100977 Drug Info Phase 2 Asthma; Chronic obstructive pulmonary disease [548577]
MN-221 Drug Info Phase 2 Aging skin; Exacerbations of acute asthma [522325]
R-salbutamol sulphate Drug Info Phase 2 Skin infections [522239]
TA-2005 Drug Info Phase 2 Chronic obstructive pulmonary disease [536223]
THRX-198321 Drug Info Phase 2 Chronic obstructive pulmonary disease [549872]
KUL-7211 Drug Info Phase 1 Neurogenic bladder dysfunction [547180]
L-796568 Drug Info Phase 1 Obesity [526432]
Meluadrine Drug Info Discontinued in Preregistration Premature ejaculation [545398]
Broxaterol Drug Info Discontinued in Phase 3 Asthma [544547]
Sibenadet Drug Info Discontinued in Phase 3 Chronic obstructive pulmonary disease [536661]
GSK-159797 Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [536223]
GSK159802 Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease; Asthma [548082]
Milveterol Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease; Asthma [537130]
Milveterol+Fluticasone Drug Info Discontinued in Phase 2 Asthma; Chronic obstructive pulmonary disease [550969]
PF-610355 Drug Info Discontinued in Phase 2 Asthma; Chronic obstructive pulmonary disease [548443]
Picumeterol Drug Info Discontinued in Phase 2 Bronchodilator [545347]
AR-C-89855 Drug Info Terminated Chronic obstructive pulmonary disease [547129]
L-755507 Drug Info Terminated Discovery agent [540554], [546489]
RP-58802B Drug Info Terminated Asthma [544951]
Inhibitor (R,R)-(-)-fenoterol Drug Info [528842]
(R,S)-(-)-fenoterol Drug Info [528842]
(S,R)-(+)-fenoterol Drug Info [528842]
1-(2-allylphenoxy)-3-morpholinopropan-2-ol Drug Info [530883]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol Drug Info [530883]
2-fluoronorepinehprine Drug Info [530478]
CGP-12177A Drug Info [526033]
DICHLOROISOPROTERENOL Drug Info [533801]
GNF-PF-1694 Drug Info [529732]
L-755507 Drug Info [526033]
L-796568 Drug Info [530748]
SDZ-201106 Drug Info [529732]
Agonist APD-209 Drug Info [544329]
AR-C-89855 Drug Info [547130]
Arformoterol Drug Info [535891], [537134]
AZD-2115 Drug Info [532016]
AZD-3199 Drug Info [544464]
Bambuterol Drug Info [536563]
Carmoterol Drug Info [537130]
Clenbuterol Drug Info [535304], [536989]
D 2343 Drug Info [537806]
Fenoterol Drug Info [535311], [537192]
Formoterol Drug Info [534986], [535115], [535518]
GSK-159797 Drug Info [536223]
GSK159802 Drug Info [550963]
GSK642444 Drug Info [532150], [532651], [537130]
GW642444 Drug Info [550963]
Indacaterol Drug Info [536223], [537130]
Isoprenaline Drug Info [538095]
LAS 100977 Drug Info [531905]
Milveterol Drug Info [550963]
Milveterol+Fluticasone Drug Info [537130]
MN-221 Drug Info [530213]
Orciprenaline Drug Info [536544]
PF-610355 Drug Info [531136]
Picumeterol Drug Info [534374]
Pirbuterol Drug Info [536347], [536442]
Procaterol Drug Info [535606], [536454]
PT005 Drug Info [551485]
QVA-149 Drug Info [537130]
R-salbutamol sulphate Drug Info [534530]
Salbutamol Drug Info [535331]
Salmeterol Drug Info [536966]
TA-2005 Drug Info [536223]
Terbutaline Drug Info [537680]
Modulator Broxaterol Drug Info [533154]
BUCINDOLOL Drug Info
GSK961081 Drug Info
Isoetharine Drug Info [556264]
Isoproterenol Drug Info [556264]
KUL-7211 Drug Info [526702]
Meluadrine Drug Info [526451]
Metaproterenol Sulfate Drug Info [556264]
Olodaterol Drug Info [533123]
Ritodrine Drug Info [556264]
RP-58802B Drug Info [526640]
salbutamol dry-powder inhalation Drug Info
Sibenadet Drug Info
THRX-198321 Drug Info [531285]
Vilanterol Drug Info [542374]
Antagonist Butoxamine Drug Info [535096]
ICI 118,551 Drug Info [537716]
Levalbuterol Drug Info [537409]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Endocytosis
Adrenergic signaling in cardiomyocytes
Salivary secretion
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Beta2 adrenergic receptor signaling pathway
Pathway Interaction Database Arf6 trafficking events
Arf6 signaling events
Reactome Adrenoceptors
G alpha (s) signalling events
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
References
Ref 522239ClinicalTrials.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 522325ClinicalTrials.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 522407ClinicalTrials.gov (NCT00736489) Single-dose Crossover Study to Investigate Pharmacodynamics of AZD3199. U.S. National Institutes of Health.
Ref 524423ClinicalTrials.gov (NCT01936649) Open-label, Test-retest Study Assessing Reproducibility of Quantitative Measurements of Myocardial Uptake of AdreView.. U.S. National Institutes of Health.
Ref 524493ClinicalTrials.gov (NCT01970501) Genetically Targeted Therapy for the Prevention of Symptomatic Atrial Fibrillation in Patients With Heart Failure. U.S. National Institutes of Health.
Ref 524508ClinicalTrials.gov (NCT01977443) Therapeutic Efficacy of APD-209 Eye Drops in Treatment of Epidemic Keratoconjunctivitis (EKC). U.S. National Institutes of Health.
Ref 524708ClinicalTrials.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 525067ClinicalTrials.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 526432Effect 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 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 532150Vilanterol 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 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536500Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
Ref 536535Long duration of airway but not systemic effects of inhaled formoterol in asthmatic patients. Respir Med. 2008 Mar;102(3):449-56. Epub 2007 Nov 19.
Ref 536567Acute clenbuterol overdose resulting in supraventricular tachycardia and atrial fibrillation. J Med Toxicol. 2007 Jun;3(2):56-60.
Ref 536661Anti-obesity drugs and neural circuits of feeding. Trends Pharmacol Sci. 2008 Apr;29(4):208-17. Epub 2008 Mar 18.
Ref 537130Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94.
Ref 538236FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071438.
Ref 538303FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075877.
Ref 538350FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083346.
Ref 538363FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 086711.
Ref 540402(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: 3464).
Ref 540403(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: 3465).
Ref 540554(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: 3931).
Ref 540946(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: 557).
Ref 540951(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: 558).
Ref 540957(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: 559).
Ref 540968(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: 560).
Ref 541721(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: 6601).
Ref 542219(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: 7205).
Ref 542268(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: 7250).
Ref 542292(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: 7272).
Ref 542314(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: 7294).
Ref 542374(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: 7353).
Ref 542479(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: 7455).
Ref 542501(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 542545(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: 7543).
Ref 542572(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: 7582).
Ref 544547Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000105)
Ref 544951Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001694)
Ref 545347Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002942)
Ref 545398Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003111)
Ref 545941Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005434)
Ref 546489Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008526)
Ref 547129Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013263)
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 548082Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021784)
Ref 548296Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024247)
Ref 548443Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025582)
Ref 548577Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026746)
Ref 549872Clinical pipeline report, company report or official report of Theravance.
Ref 550662Drug information of Orciprenaline, 2008. eduDrugs.
Ref 550744Drug information of Clenbuterol, 2008. eduDrugs.
Ref 550747Drug information of Procaterol, 2008. eduDrugs.
Ref 550969Clinical pipeline report, company report or official report of GlaxoSmithKline.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551966Clinical pipeline report, company report or official report of Novartis.
Ref 526033J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.
Ref 526451Effects 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 526640RP 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 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 528842J 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.
Ref 529732Bioorg 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.
Ref 530213Investigation 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 530478Bioorg 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.
Ref 530748Bioorg 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.
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 531136Inhalation 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 531285THRX-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 531905Pharmacological 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 532016Evaluation of WO-2012085582 and WO-2012085583 two identified MABAs: backups to AZD-2115. Expert Opin Ther Pat. 2012 Nov;22(11):1377-83.
Ref 532150Vilanterol 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 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 533154Broxaterol, a new beta 2-adrenoceptor agonist compared to salbutamol in asthmatics, oral and inhalation treatment. Respiration. 1989;55 Suppl 2:15-9.
Ref 533801J 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.
Ref 534374Picumeterol: dissociation of improvement in lung function and reduction of airways hyperresponsiveness in asthmatics. Br J Clin Pharmacol. 1997 Feb;43(2):169-76.
Ref 534530Pharmacokinetics 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 534986Long-acting beta2-agonists for chronic obstructive pulmonary disease. Cochrane Database Syst Rev. 2000;(2):CD001104.
Ref 535096Partial agonistic effects of carteolol on atypical beta-adrenoceptors in the guinea pig gastric fundus. Jpn J Pharmacol. 2000 Nov;84(3):287-92.
Ref 535115Tocolytic effects of a long-acting beta2-adrenoceptor agonist, formoterol, in rats. J Pharm Pharmacol. 2000 Nov;52(11):1417-23.
Ref 535304Beta(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 535311Effect 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 535331Potential of beta2-adrenoceptor agonists as add-on therapy for multiple sclerosis: focus on salbutamol (albuterol). CNS Drugs. 2002;16(1):1-8.
Ref 535518Long-acting beta2-agonists for chronic obstructive pulmonary disease patients with poorly reversible airflow limitation. Cochrane Database Syst Rev. 2002;(3):CD001104.
Ref 535606beta 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 535891Arformoterol: (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 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 536347A 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.
Ref 536442Inhaled beta agonists. Respir Care. 2007 Jul;52(7):820-32.
Ref 536454Inhalation and incubation with procaterol increases diaphragm muscle contractility in mice. Allergol Int. 2007 Sep;56(3):285-91. Epub 2007 Aug 1.
Ref 536544Male--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.
Ref 536563Enantiomeric separation of beta2-agonists on macrocyclic antibiotic chiral stationary phases in high performance liquid chromatography. Pharmazie. 2007 Nov;62(11):836-40.
Ref 536966Pharmacogenetic tests in asthma therapy. Clin Lab Med. 2008 Dec;28(4):645-65.
Ref 536989Postischemic brain injury is attenuated in mice lacking the beta2-adrenergic receptor. Anesth Analg. 2009 Jan;108(1):280-7.
Ref 537130Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94.
Ref 537134Arformoterol tartrate in the treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease. Drugs Today (Barc). 2009 Jan;45(1):3-9.
Ref 537192Functional alpha1- and beta2-adrenergic receptors in human osteoblasts. J Cell Physiol. 2009 Jul;220(1):267-75.
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