Target Information

Target General Infomation
Target ID
T44068
Former ID
TTDS00036
Target Name
Beta-1 adrenergic receptor
Gene Name
ADRB1
Synonyms
Beta-1 adrenoceptor; Beta-1 adrenoreceptor; ADRB1
Target Type
Successful
Disease Angina pectoris; Hypertension [ICD9:413, 401; ICD10: I20, I10-I16]
Angina pectoris [ICD9: 413; ICD10: I20]
Acute supraventricular tachycardia [ICD9: 427.0, 427.89; ICD10: I47.1]
Allergy; Sepsis [ICD9:995.3, 995.91; ICD10: T78.4, A40, A41]
Bronchodilator [ICD9: 493; ICD10: J45]
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49]
Chronic open-angle glaucoma [ICD10: H40]
Chronic open-angle glaucoma; Ocular hypertension [ICD10: H40]
Central and peripheral nervous diseases [ICD10: G96.9]
Circulatory disorders [ICD10: I00-I99]
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Hypertension; Ventricular premature beats [ICD10: I10-I16]
High blood pressure; Angina [ICD9: 401, 413; ICD10: I10, I11, I12, I13, I15, I20]
Hypertension [ICD9: 401; ICD10: I10-I16]
Hypertension; Angina [ICD9: 401, 413; ICD10: I10-I16, I20]
Hypertension; Heart arrhythmia [ICD9:401; ICD10: I10-I16, I47-I49]
High blood pressure [ICD9: 401; ICD10: I10-I16]
Heart failure; Cardiogenic shock [ICD9: 428.0, 785.51; ICD10: I50, R57.0]
Heart failure [ICD9: 428; ICD10: I50]
Hypertension; Angina pectoris [ICD9:401, 413; ICD10: I10-I16, I20]
Maintenance of normal sinus rhythm [ICD9: 427; ICD10: I46-I49]
Migraine [ICD9: 346; ICD10: G43]
Obesity [ICD9: 278; ICD10: E66]
Open-angle glaucoma [ICD9: 365; ICD10: H40-H42]
Open-angle glaucoma; Ocular hypertension [ICD9: 365, 365.04; ICD10: H40-H42, H40.0]
Septic shock; Neurogenic shock [ICD9: 785, 785.52; ICD10: R57.8, R65.21]
Ventricular fibrillation [ICD10: I49.01]
Function
Beta-adrenergic receptors mediatethe catecholamine- induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
BioChemical Class
GPCR rhodopsin
Target Validation
T44068
UniProt ID
P08588
Sequence
MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV
WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC
TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM
AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP
LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV
FFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGP
PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV
Structure
2LSQ
Drugs and Mode of Action
Drug(s) Acebutolol Drug Info Approved Hypertension; Ventricular premature beats [1]
Ajmalicine Drug Info Approved Circulatory disorders [1]
Anisodamine Drug Info Approved Central and peripheral nervous diseases [1]
Anisodine Drug Info Approved Central and peripheral nervous diseases [1]
Arbutamine Drug Info Approved Coronary artery disease [2]
Atenolol Drug Info Approved Hypertension [3], [4]
Betaxolol Drug Info Approved Hypertension [5], [6]
Bethanidine Drug Info Approved Hypertension; Heart arrhythmia [7], [8], [1]
Bisoprolol Drug Info Approved Hypertension [5], [9]
Bretylium Drug Info Approved Ventricular fibrillation [1]
Carteolol Drug Info Approved Glaucoma [1]
Dipivefrin Drug Info Approved Chronic open-angle glaucoma [1]
Dobutamine Drug Info Approved Heart failure; Cardiogenic shock [10], [11]
Epinephrine Drug Info Approved Allergy; Sepsis [12], [1], [13]
Esmolol Drug Info Approved Acute supraventricular tachycardia [5], [14]
Levobetaxolol Drug Info Approved Chronic open-angle glaucoma; Ocular hypertension [1]
Levobunolol Drug Info Approved Open-angle glaucoma [5], [15]
Metipranolol Drug Info Approved Open-angle glaucoma; Ocular hypertension [16], [17], [1]
Metoprolol Drug Info Approved Angina pectoris; Hypertension [18], [19], [20]
Nadolol Drug Info Approved High blood pressure; Angina [21], [22]
Nebivolol Drug Info Approved Hypertension [5], [23]
Norepinephrine Drug Info Approved Septic shock; Neurogenic shock [24], [25]
Oxprenolol Drug Info Approved Angina pectoris; Hypertension [26], [27], [28], [29]
Penbutolol Drug Info Approved Hypertension; Angina pectoris [30], [31], [1]
Pindolol Drug Info Approved Hypertension; Angina [32], [33]
Practolol Drug Info Approved Cardiac arrhythmias [34], [35]
Propranolol Drug Info Approved Migraine [36], [37]
Protokylol Hydrochloride Drug Info Approved Bronchodilator [1]
Sotalol Drug Info Approved Maintenance of normal sinus rhythm [38], [39]
Timolol Drug Info Approved High blood pressure [40], [41]
BRL 35135 Drug Info Phase 2 Diabetes [42], [43]
BUCINDOLOL Drug Info Phase 2 Hypertension [44]
COR-1 Drug Info Phase 2 Heart failure [45]
L-796568 Drug Info Phase 1 Obesity [46]
YM-16151-4 Drug Info Phase 1 Hypertension [47]
Alprenolol Drug Info Withdrawn from market Hypertension [48], [49]
Cetamolol Drug Info Terminated Angina pectoris [50]
L-755507 Drug Info Terminated Discovery agent [51], [52]
Inhibitor (+/-)-nantenine Drug Info [53]
(R,R)-(-)-fenoterol Drug Info [54]
(R,S)-(-)-fenoterol Drug Info [54]
1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol Drug Info [55]
1-(2-allylphenoxy)-3-morpholinopropan-2-ol Drug Info [56]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol Drug Info [56]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [57]
CGP-12177A Drug Info [58]
DICHLOROISOPROTERENOL Drug Info [59]
L-755507 Drug Info [58]
L-796568 Drug Info [60]
Antagonist Acebutolol Drug Info [61], [62]
Alprenolol Drug Info [63], [64]
Atenolol Drug Info [61], [62]
Betaxolol Drug Info [65], [66]
Bethanidine Drug Info [67]
Bisoprolol Drug Info [68], [69]
Bretylium Drug Info [70], [71]
Cebutolol Drug Info [62]
CGP 20712A Drug Info [72]
CGP 26505 Drug Info [73]
COR-1 Drug Info [45]
Dipivefrin Drug Info [74]
Esmolol Drug Info [75]
Levobetaxolol Drug Info [76]
Levobunolol Drug Info [77]
Metipranolol Drug Info [78]
Metoprolol Drug Info [79], [61], [62]
Nebivolol Drug Info [80]
Oxprenolol Drug Info [61]
Penbutolol Drug Info [81], [82]
Pindolol Drug Info [83]
Practolol Drug Info [84], [34]
Propranolol Drug Info [85]
Sotalol Drug Info [86]
Timolol Drug Info [87], [88], [89]
Modulator Ajmalicine Drug Info [90]
Anisodamine Drug Info [90]
Anisodine Drug Info [90]
BUCINDOLOL Drug Info
Cetamolol Drug Info [45], [91]
Nadolol Drug Info [92]
Protokylol Hydrochloride Drug Info
YM-16151-4 Drug Info [47]
Stimulator Arbutamine Drug Info [93]
Norepinephrine Drug Info [94]
Agonist BRL 35135 Drug Info [95]
Carazolol Drug Info [62]
Carteolol Drug Info [96], [97]
Dobutamine Drug Info [98], [69]
Epinephrine Drug Info [99]
Isoprenaline Drug Info [62]
Noradrenaline Drug Info [100]
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Endocytosis
Adrenergic signaling in cardiomyocytes
Gap junction
Salivary secretion
Dilated cardiomyopathy
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Beta1 adrenergic receptor signaling pathway
PathWhiz Pathway Muscle/Heart Contraction
Reactome Adrenoceptors
G alpha (s) signalling events
WikiPathways Monoamine GPCRs
Calcium Regulation in the Cardiac Cell
GPCRs, Class A Rhodopsin-like
Endothelin Pathways
GPCR ligand binding
GPCR downstream signaling
References
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