Target Information

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; 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]
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]
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 labour [ICD9: 644, 765; ICD10: O60.1, P07.3]
Premature ejaculation [ICD9: 302.75; ICD10: F52.4]
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
P07550
Sequence
MGQPGNGSAFLLAPNGSHAPDHDVTQERDEVWVVGMGIVMSLIVLAIVFGNVLVITAIAK
FERLQTVTNYFITSLACADLVMGLAVVPFGAAHILMKMWTFGNFWCEFWTSIDVLCVTAS
IETLCVIAVDRYFAITSPFKYQSLLTKNKARVIILMVWIVSGLTSFLPIQMHWYRATHQE
AINCYANETCCDFFTNQAYAIASSIVSFYVPLVIMVFVYSRVFQEAKRQLQKIDKSEGRF
HVQNLSQVEQDGRTGHGLRRSSKFCLKEHKALKTLGIIMGTFTLCWLPFFIVNIVHVIQD
NLIRKEVYILLNWIGYVNSGFNPLIYCRSPDFRIAFQELLCLRRSSLKAYGNGYSSNGNT
GEQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSQGRNCSTNDSLL
Drugs and Mode of Action
Drug(s) Arformoterol Drug Info Approved Chronic obstructive pulmonary disease [1], [2]
Bambuterol Drug Info Approved Asthma [3], [4]
Clenbuterol Drug Info Approved Chronic breathing disorders [5]
Fenoterol Drug Info Approved Asthma [6], [7]
Formoterol Drug Info Approved Asthma [8], [9]
GW642444 Drug Info Approved Asthma [10], [11]
Indacaterol Drug Info Approved Chronic obstructive pulmonary disease [12], [13]
Isoetharine Drug Info Approved Asthma [14], [15]
Isoproterenol Drug Info Approved Bradycardia; Heart block [16]
Levalbuterol Drug Info Approved Asthma [17], [18]
Metaproterenol Sulfate Drug Info Approved Asthma [18]
Olodaterol Drug Info Approved Chronic obstructive pulmonary disease [19], [20]
Orciprenaline Drug Info Approved Asthma [21], [22]
Pirbuterol Drug Info Approved Asthma [3], [23]
Procaterol Drug Info Approved Asthma [24], [25]
Ritodrine Drug Info Approved Premature labour [26], [27]
Salbutamol Drug Info Approved Acute asthma [28], [29]
Salmeterol Drug Info Approved Chronic obstructive pulmonary disease [3], [30]
Terbutaline Drug Info Approved Asthma [31], [32]
Vilanterol Drug Info Approved Asthma; Chronic obstructive pulmonary disease [33], [34], [18]
GSK642444 Drug Info Phase 3 Chronic obstructive pulmonary disease [35]
PT005 Drug Info Phase 3 Chronic obstructive pulmonary disease [36]
QVA-149 Drug Info Phase 3 Chronic obstructive pulmonary disease [37]
APD-209 Drug Info Phase 2 Cachexia [38]
AZD-2115 Drug Info Phase 2 Chronic obstructive pulmonary disease [39]
AZD-3199 Drug Info Phase 2 Asthma [40]
BUCINDOLOL Drug Info Phase 2 Hypertension [41]
Carmoterol Drug Info Phase 2 Chronic obstructive pulmonary disease [35], [42]
GSK961081 Drug Info Phase 2 Chronic obstructive pulmonary disease [43]
LAS 100977 Drug Info Phase 2 Asthma; Chronic obstructive pulmonary disease [44]
MN-221 Drug Info Phase 2 Aging skin; Exacerbations of acute asthma [45]
R-salbutamol sulphate Drug Info Phase 2 Skin infections [46]
TA-2005 Drug Info Phase 2 Chronic obstructive pulmonary disease [1]
THRX-198321 Drug Info Phase 2 Chronic obstructive pulmonary disease [47]
KUL-7211 Drug Info Phase 1 Neurogenic bladder dysfunction [48]
L-796568 Drug Info Phase 1 Obesity [49]
Meluadrine Drug Info Discontinued in Preregistration Premature ejaculation [50]
Broxaterol Drug Info Discontinued in Phase 3 Asthma [51]
Sibenadet Drug Info Discontinued in Phase 3 Chronic obstructive pulmonary disease [52]
GSK-159797 Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [1]
GSK159802 Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease; Asthma [53]
Milveterol Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease; Asthma [35]
Milveterol+Fluticasone Drug Info Discontinued in Phase 2 Asthma; Chronic obstructive pulmonary disease [54]
PF-610355 Drug Info Discontinued in Phase 2 Asthma; Chronic obstructive pulmonary disease [55]
Picumeterol Drug Info Discontinued in Phase 2 Bronchodilator [56]
AR-C-89855 Drug Info Terminated Chronic obstructive pulmonary disease [57]
L-755507 Drug Info Terminated Discovery agent [58], [59]
RP-58802B Drug Info Terminated Asthma [60]
Inhibitor (R,R)-(-)-fenoterol Drug Info [61]
(R,S)-(-)-fenoterol Drug Info [61]
(S,R)-(+)-fenoterol Drug Info [61]
1-(2-allylphenoxy)-3-morpholinopropan-2-ol Drug Info [62]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol Drug Info [62]
2-fluoronorepinehprine Drug Info [63]
CGP-12177A Drug Info [64]
DICHLOROISOPROTERENOL Drug Info [65]
GNF-PF-1694 Drug Info [66]
L-755507 Drug Info [64]
L-796568 Drug Info [67]
SDZ-201106 Drug Info [66]
Agonist APD-209 Drug Info [68]
AR-C-89855 Drug Info [69]
Arformoterol Drug Info [70], [71]
AZD-2115 Drug Info [72]
AZD-3199 Drug Info [73]
Bambuterol Drug Info [74]
Carmoterol Drug Info [35]
Clenbuterol Drug Info [75], [76]
D 2343 Drug Info [77]
Fenoterol Drug Info [78], [79]
Formoterol Drug Info [80], [81], [82]
GSK-159797 Drug Info [1]
GSK159802 Drug Info [83]
GSK642444 Drug Info [10], [11], [35]
GW642444 Drug Info [83]
Indacaterol Drug Info [1], [35]
Isoprenaline Drug Info [84]
LAS 100977 Drug Info [85]
Milveterol Drug Info [83]
Milveterol+Fluticasone Drug Info [35]
MN-221 Drug Info [86]
Orciprenaline Drug Info [87]
PF-610355 Drug Info [88]
Picumeterol Drug Info [89]
Pirbuterol Drug Info [90], [91]
Procaterol Drug Info [92], [93]
PT005 Drug Info [94]
QVA-149 Drug Info [35]
R-salbutamol sulphate Drug Info [95]
Salbutamol Drug Info [96]
Salmeterol Drug Info [97]
TA-2005 Drug Info [1]
Terbutaline Drug Info [98]
Modulator Broxaterol Drug Info [99]
BUCINDOLOL Drug Info
GSK961081 Drug Info
Isoetharine Drug Info [100]
Isoproterenol Drug Info [100]
KUL-7211 Drug Info [101]
Meluadrine Drug Info [102]
Metaproterenol Sulfate Drug Info [100]
Olodaterol Drug Info [19]
Ritodrine Drug Info [100]
RP-58802B Drug Info [103]
salbutamol dry-powder inhalation Drug Info
Sibenadet Drug Info
THRX-198321 Drug Info [104]
Vilanterol Drug Info [34]
Antagonist Butoxamine Drug Info [105]
ICI 118,551 Drug Info [106]
Levalbuterol Drug Info [107]
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
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REF 2(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 3Natural 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 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: 6601).
REF 5Drug information of Clenbuterol, 2008. eduDrugs.
REF 6Acute clenbuterol overdose resulting in supraventricular tachycardia and atrial fibrillation. J Med Toxicol. 2007 Jun;3(2):56-60.
REF 7(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 8Long 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.
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REF 10Vilanterol 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.
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REF 16FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083346.
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REF 22Drug information of Orciprenaline, 2008. eduDrugs.
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: 7272).
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REF 25Drug information of Procaterol, 2008. eduDrugs.
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REF 31FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075877.
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REF 46ClinicalTrials.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 47Clinical pipeline report, company report or official report of Theravance.
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