Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T44068
(Former ID: TTDS00036)
|
|||||
Target Name |
Adrenergic receptor beta-1 (ADRB1)
|
|||||
Synonyms |
Beta-1 adrenoreceptor; Beta-1 adrenoceptor; Beta-1 adrenergic receptor; B1AR; ADRB1R
|
|||||
Gene Name |
ADRB1
|
|||||
Target Type |
Successful target
|
[1] | ||||
Disease | [+] 15 Target-related Diseases | + | ||||
1 | Allergic/hypersensitivity disorder [ICD-11: 4A80-4A8Z] | |||||
2 | Asthma [ICD-11: CA23] | |||||
3 | Cardiac arrhythmia [ICD-11: BC9Z] | |||||
4 | Central and peripheral nervous disease [ICD-11: 8A04-8E7Z] | |||||
5 | Circulatory system disease [ICD-11: BE2Z] | |||||
6 | Conduction disorder [ICD-11: BC63] | |||||
7 | Coronary atherosclerosis [ICD-11: BA80] | |||||
8 | Essential hypertension [ICD-11: BA00] | |||||
9 | Glaucoma [ICD-11: 9C61] | |||||
10 | Heart failure [ICD-11: BD10-BD1Z] | |||||
11 | Hypertension [ICD-11: BA00-BA04] | |||||
12 | Migraine [ICD-11: 8A80] | |||||
13 | Sepsis [ICD-11: 1G40-1G41] | |||||
14 | Supraventricular tachyarrhythmia [ICD-11: BC81] | |||||
15 | Ventricular tachyarrhythmia [ICD-11: BC71] | |||||
Function |
Beta-adrenergic receptors mediate the 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.
Click to Show/Hide
|
|||||
BioChemical Class |
GPCR rhodopsin
|
|||||
UniProt ID | ||||||
Sequence |
MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV FFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGP PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A02934 | |||||
HIT2.0 ID | T64T6J |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Approved Drug(s) | [+] 30 Approved Drugs | + | ||||
1 | Acebutolol | Drug Info | Approved | Hypertension | [2] | |
2 | Ajmalicine | Drug Info | Approved | Circulatory disorder | [2] | |
3 | Anisodamine | Drug Info | Approved | Central and peripheral nervous disease | [2] | |
4 | Anisodine | Drug Info | Approved | Central and peripheral nervous disease | [2] | |
5 | Arbutamine | Drug Info | Approved | Coronary artery disease | [3] | |
6 | Atenolol | Drug Info | Approved | Hypertension | [4], [5] | |
7 | Betaxolol | Drug Info | Approved | Hypertension | [6], [7] | |
8 | Bisoprolol | Drug Info | Approved | Hypertension | [7], [8] | |
9 | Bretylium | Drug Info | Approved | Ventricular fibrillation | [2] | |
10 | Carteolol | Drug Info | Approved | Glaucoma/ocular hypertension | [2] | |
11 | Dipivefrin | Drug Info | Approved | Chronic open-angle glaucoma | [2] | |
12 | Dobutamine | Drug Info | Approved | Heart failure | [9], [10] | |
13 | Epinephrine | Drug Info | Approved | Allergy | [2], [11], [12] | |
14 | Esmolol | Drug Info | Approved | Acute supraventricular tachycardia | [13], [7] | |
15 | Isoproterenol | Drug Info | Approved | Heart block | [14] | |
16 | Levobetaxolol | Drug Info | Approved | Chronic open-angle glaucoma | [2] | |
17 | Levobunolol | Drug Info | Approved | Open-angle glaucoma | [15], [7] | |
18 | Metipranolol | Drug Info | Approved | Open-angle glaucoma | [2], [16], [17] | |
19 | Metoprolol | Drug Info | Approved | Hypertension | [18], [19], [20] | |
20 | Nadolol | Drug Info | Approved | High blood pressure | [21], [22] | |
21 | Nebivolol | Drug Info | Approved | Hypertension | [23], [7] | |
22 | Norepinephrine | Drug Info | Approved | Sepsis | [24], [25] | |
23 | Oxprenolol | Drug Info | Approved | Hypertension | [26], [27], [28], [29] | |
24 | Penbutolol | Drug Info | Approved | Hypertension | [30], [31], [2] | |
25 | Pindolol | Drug Info | Approved | Hypertension | [32], [33] | |
26 | Practolol | Drug Info | Approved | Cardiac arrhythmias | [34], [35] | |
27 | Propranolol | Drug Info | Approved | Migraine | [36], [37] | |
28 | Protokylol Hydrochloride | Drug Info | Approved | Asthma | [2] | |
29 | Sotalol | Drug Info | Approved | Sinus rhythm disorder | [38], [39] | |
30 | Timolol | Drug Info | Approved | High blood pressure | [40], [41] | |
Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
1 | BUCINDOLOL | Drug Info | Phase 2/3 | Atrial fibrillation | [42] | |
2 | BRL 35135 | Drug Info | Phase 2 | Diabetic complication | [43], [44] | |
3 | COR-1 | Drug Info | Phase 2 | Heart failure | [45] | |
4 | Galnobax | Drug Info | Phase 1/2 | Diabetic foot ulcer | [46], [47] | |
5 | L-796568 | Drug Info | Phase 1 | Obesity | [48] | |
6 | YM-16151-4 | Drug Info | Phase 1 | Hypertension | [49] | |
Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
1 | Alprenolol | Drug Info | Withdrawn from market | Hypertension | [50], [51] | |
2 | Bethanidine | Drug Info | Withdrawn from market | Heart arrhythmia | [52] | |
3 | Cetamolol | Drug Info | Terminated | Angina pectoris | [53] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Antagonist | [+] 24 Antagonist drugs | + | ||||
1 | Acebutolol | Drug Info | [54], [55] | |||
2 | Atenolol | Drug Info | [54], [55] | |||
3 | Betaxolol | Drug Info | [58], [59] | |||
4 | Bisoprolol | Drug Info | [60], [61] | |||
5 | Bretylium | Drug Info | [62], [63] | |||
6 | Dipivefrin | Drug Info | [66] | |||
7 | Esmolol | Drug Info | [69] | |||
8 | Levobetaxolol | Drug Info | [70] | |||
9 | Levobunolol | Drug Info | [1] | |||
10 | Metipranolol | Drug Info | [71] | |||
11 | Metoprolol | Drug Info | [54], [55], [72] | |||
12 | Nebivolol | Drug Info | [74] | |||
13 | Oxprenolol | Drug Info | [54] | |||
14 | Penbutolol | Drug Info | [76], [77] | |||
15 | Pindolol | Drug Info | [78] | |||
16 | Practolol | Drug Info | [35], [79] | |||
17 | Propranolol | Drug Info | [80] | |||
18 | Sotalol | Drug Info | [82] | |||
19 | Timolol | Drug Info | [83], [84], [85] | |||
20 | COR-1 | Drug Info | [45] | |||
21 | Alprenolol | Drug Info | [91], [92] | |||
22 | Bethanidine | Drug Info | [93] | |||
23 | Cebutolol | Drug Info | [55] | |||
24 | CGP 20712A | Drug Info | [101], [102] | |||
Modulator | [+] 8 Modulator drugs | + | ||||
1 | Ajmalicine | Drug Info | [56] | |||
2 | Anisodamine | Drug Info | [56] | |||
3 | Anisodine | Drug Info | [56] | |||
4 | Nadolol | Drug Info | [73] | |||
5 | Protokylol Hydrochloride | Drug Info | [81] | |||
6 | BUCINDOLOL | Drug Info | [86], [87], [88] | |||
7 | YM-16151-4 | Drug Info | [49] | |||
8 | Cetamolol | Drug Info | [94], [45] | |||
Stimulator | [+] 2 Stimulator drugs | + | ||||
1 | Arbutamine | Drug Info | [57] | |||
2 | Norepinephrine | Drug Info | [75] | |||
Agonist | [+] 7 Agonist drugs | + | ||||
1 | Carteolol | Drug Info | [64], [65] | |||
2 | Dobutamine | Drug Info | [61], [67] | |||
3 | Epinephrine | Drug Info | [68] | |||
4 | Isoproterenol | Drug Info | [55] | |||
5 | BRL 35135 | Drug Info | [89] | |||
6 | Galnobax | Drug Info | [46] | |||
7 | Carazolol | Drug Info | [55] | |||
Inhibitor | [+] 11 Inhibitor drugs | + | ||||
1 | L-796568 | Drug Info | [90] | |||
2 | L-755507 | Drug Info | [95] | |||
3 | (+/-)-nantenine | Drug Info | [96] | |||
4 | (R,R)-(-)-fenoterol | Drug Info | [97] | |||
5 | (R,S)-(-)-fenoterol | Drug Info | [97] | |||
6 | 1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol | Drug Info | [98] | |||
7 | 1-(2-allylphenoxy)-3-morpholinopropan-2-ol | Drug Info | [99] | |||
8 | 1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol | Drug Info | [99] | |||
9 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [100] | |||
10 | Dichloroisoproterenol | Drug Info | [103] | |||
11 | [3H]CGP12177 | Drug Info | [95] |
Chemical Structure based Activity Landscape of Target | Top |
---|---|
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 | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 9 KEGG Pathways | + | ||||
1 | Calcium signaling pathway | |||||
2 | cGMP-PKG signaling pathway | |||||
3 | cAMP signaling pathway | |||||
4 | Neuroactive ligand-receptor interaction | |||||
5 | Endocytosis | |||||
6 | Adrenergic signaling in cardiomyocytes | |||||
7 | Gap junction | |||||
8 | Salivary secretion | |||||
9 | Dilated cardiomyopathy | |||||
Panther Pathway | [+] 2 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
2 | Beta1 adrenergic receptor signaling pathway | |||||
Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
1 | Muscle/Heart Contraction | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Adrenoceptors | |||||
2 | G alpha (s) signalling events | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | Monoamine GPCRs | |||||
2 | Calcium Regulation in the Cardiac Cell | |||||
3 | GPCRs, Class A Rhodopsin-like | |||||
4 | Endothelin Pathways | |||||
5 | GPCR ligand binding | |||||
6 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Binding of beta-adrenoceptor antagonists to rat and rabbit lung: special reference to levobunolol. Arzneimittelforschung. 1984;34(5):579-84. | |||||
REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 3 | Drug information of Arbutamine, 2008. eduDrugs. | |||||
REF 4 | 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: 548). | |||||
REF 5 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 072303. | |||||
REF 6 | 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: 549). | |||||
REF 7 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 8 | 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: 7129). | |||||
REF 9 | 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: 535). | |||||
REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074086. | |||||
REF 11 | 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: 509). | |||||
REF 12 | Drug information of Epinephrine, 2008. eduDrugs. | |||||
REF 13 | 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: 7178). | |||||
REF 14 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083346. | |||||
REF 15 | 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: 570). | |||||
REF 16 | 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: 7239). | |||||
REF 17 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075720. | |||||
REF 18 | 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: 553). | |||||
REF 19 | Metoprolol: a review of its use in chronic heart failure. Drugs. 2000 Sep;60(3):647-78. | |||||
REF 20 | The effect of food on the relative bioavailability of rapidly dissolving immediate-release solid oral products containing highly soluble drugs. Mol Pharm. 2004 Sep-Oct;1(5):357-62. | |||||
REF 21 | 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: 554). | |||||
REF 22 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074229. | |||||
REF 23 | 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: 7246). | |||||
REF 24 | 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: 505). | |||||
REF 25 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040455. | |||||
REF 26 | 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: 7255). | |||||
REF 27 | Controlled evaluation of the beta adrenoceptor blocking drug oxprenolol in anxiety. Med J Aust. 1976 Jun 12;1(24):909-12. | |||||
REF 28 | The beta 1- and beta 2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol: a study in the isolated right atrium and uterus of the rat. Br J Pharmacol. 1986 Apr;87(4):657-64. | |||||
REF 29 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018166. | |||||
REF 30 | 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: 7263). | |||||
REF 31 | Penbutolol and carteolol: two new beta-adrenergic blockers with partial agonism. J Clin Pharmacol. 1990 May;30(5):412-21. | |||||
REF 32 | 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: 91). | |||||
REF 33 | Report of the Canadian Hypertension Society Consensus Conference: 3. Pharmacologic treatment of hypertensive disorders in pregnancy. CMAJ. 1997 Nov 1;157(9):1245-54. | |||||
REF 34 | 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: 555). | |||||
REF 35 | Prostaglandin E2 synthesis elicited by adrenergic stimuli in guinea pig trachea is mediated primarily via activation of beta 2 adrenergic receptors. Prostaglandins. 1992 Nov;44(5):399-412. | |||||
REF 36 | 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: 7596). | |||||
REF 37 | Emerging drugs for complications of end-stage liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):159-74. | |||||
REF 38 | 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: 7297). | |||||
REF 39 | New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22. | |||||
REF 40 | 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: 565). | |||||
REF 41 | Brinzolamide/timolol fixed combination: a new ocular suspension for the treatment of open-angle glaucoma and ocular hypertension. Expert Opin Pharmacother. 2009 Aug;10(12):2015-24. | |||||
REF 42 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 43 | Acute effects of the beta 3-adrenoceptor agonist, BRL 35135, on tissue glucose utilisation. Br J Pharmacol. 1995 Feb;114(4):888-94. | |||||
REF 44 | Biphasic effects of the beta-adrenoceptor agonist, BRL 37344, on glucose utilization in rat isolated skeletal muscle. Br J Pharmacol. 1996 Mar;117(6):1355-61. | |||||
REF 45 | Administration of the cyclic peptide COR-1 in humans (phase I study): ex vivo measurements of anti-beta1-adrenergic receptor antibody neutralization and of immune parameters. Eur J Heart Fail. 2012 Nov;14(11):1230-9. | |||||
REF 46 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 47 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 48 | 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 49 | Antianginal effects of YM-16151-4 in various experimental angina models. J Cardiovasc Pharmacol. 1993 May;21(5):701-8. | |||||
REF 50 | 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: 563). | |||||
REF 51 | Drug information of Alprenolol, 2008. eduDrugs. | |||||
REF 52 | FDA Approved Drug Products from FDA Official Website. 1981. Application Number: (ANDA) 008102. | |||||
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 800000160) | |||||
REF 54 | Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6. | |||||
REF 55 | Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404. | |||||
REF 56 | Medicinal plants in therapy. Bull World Health Organ. 1985;63(6):965-81. | |||||
REF 57 | Characterization of the adrenergic activity of arbutamine, a novel agent for pharmacological stress testing. Cardiovasc Drugs Ther. 1996 Mar;10(1):39-47. | |||||
REF 58 | beta-adrenergic enhancement of brain kynurenic acid production mediated via cAMP-related protein kinase A signaling. Prog Neuropsychopharmacol Biol Psychiatry. 2009 Apr 30;33(3):519-29. | |||||
REF 59 | Betaxolol, a beta(1)-adrenoceptor antagonist, reduces Na(+) influx into cortical synaptosomes by direct interaction with Na(+) channels: comparison with other beta-adrenoceptor antagonists. Br J Pharmacol. 2000 Jun;130(4):759-66. | |||||
REF 60 | Antiarrhythmic effect of bisoprolol, a highly selective beta1-blocker, in patients with paroxysmal atrial fibrillation. Int Heart J. 2008 May;49(3):281-93. | |||||
REF 61 | Autoimmunity in idiopathic dilated cardiomyopathy. Characterization of antibodies against the beta 1-adrenoceptor with positive chronotropic effect. Circulation. 1994 Jun;89(6):2760-7. | |||||
REF 62 | Components of functional sympathetic control of heart rate in neonatal rats. Am J Physiol. 1985 May;248(5 Pt 2):R601-10. | |||||
REF 63 | Dissociation of autonomic controls of heart rate in weaning-aged borderline hypertensive rats by perinatal NaCl. J Auton Nerv Syst. 1990 Mar;29(3):219-26. | |||||
REF 64 | 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 65 | Effects of prolonged treatment with beta-adrenoceptor antagonist, carteolol on systemic and regional hemodynamics in stroke-prone spontaneously hypertensive rats. J Pharmacobiodyn. 1991 Feb;14(2):94-100. | |||||
REF 66 | Contractile response of the isolated trabecular meshwork and ciliary muscle to cholinergic and adrenergic agents. Ger J Ophthalmol. 1996 May;5(3):146-53. | |||||
REF 67 | Beta-adrenoceptor alterations coupled with secretory response and experimental periodontitis in rat submandibular glands. Arch Oral Biol. 2008 Jun;53(6):509-16. | |||||
REF 68 | Adrenergic activation of electrogenic K+ secretion in guinea pig distal colonic epithelium: involvement of beta1- and beta2-adrenergic receptors. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G269-77. | |||||
REF 69 | Beta-1 selective adrenergic antagonist landiolol and esmolol can be safely used in patients with airway hyperreactivity. Heart Lung. 2009 Jan-Feb;38(1):48-55. | |||||
REF 70 | Binding affinities of ocular hypotensive beta-blockers levobetaxolol, levobunolol, and timolol at endogenous guinea pig beta-adrenoceptors. J Ocul Pharmacol Ther. 2004 Apr;20(2):93-9. | |||||
REF 71 | Invited review: Neuroprotective properties of certain beta-adrenoceptor antagonists used for the treatment of glaucoma. J Ocul Pharmacol Ther. 2005 Jun;21(3):175-81. | |||||
REF 72 | Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | |||||
REF 73 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 74 | Nitric oxide mechanisms of nebivolol. Ther Adv Cardiovasc Dis. 2009 Aug;3(4):317-27. | |||||
REF 75 | Impact of exogenous beta-adrenergic receptor stimulation on hepatosplanchnic oxygen kinetics and metabolic activity in septic shock. Crit Care Med. 1999 Feb;27(2):325-31. | |||||
REF 76 | beta-Adrenergic receptor blockers--a group of chiral drugs: different effects of each enantiomer. Ceska Slov Farm. 2002 May;51(3):121-8. | |||||
REF 77 | Decrease in penbutolol central response as a cause of changes in its serum protein binding. J Pharm Pharmacol. 1990 Mar;42(3):164-6. | |||||
REF 78 | Are we misunderstanding beta-blockers. Int J Cardiol. 2007 Aug 9;120(1):10-27. | |||||
REF 79 | TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. | |||||
REF 80 | Beta-blockers in the treatment of hypertension: are there clinically relevant differences Postgrad Med. 2009 May;121(3):90-8. | |||||
REF 81 | N-Aralkyl substitution increases the affinity of adrenergic drugs for the alpha-adrenoceptor in rat liver. | |||||
REF 82 | beta(2)-adrenoceptors are critical for antidepressant treatment of neuropathic pain. Ann Neurol. 2009 Feb;65(2):218-25. | |||||
REF 83 | Topical dorzolamide 2%/timolol 0.5% ophthalmic solution: a review of its use in the treatment of glaucoma and ocular hypertension. Drugs Aging. 2006;23(12):977-95. | |||||
REF 84 | Blockade of beta-adrenergic receptors prevents amphetamine-induced behavioural sensitization in rats: a putative role of the bed nucleus of the str... Int J Neuropsychopharmacol. 2005 Dec;8(4):569-81. | |||||
REF 85 | A prospective study of the effects of prolonged timolol therapy on alpha- and beta-adrenoceptor and angiotensin II receptor mediated responses in normal subjects. Br J Clin Pharmacol. 1997 Mar;43(3):301-8. | |||||
REF 86 | Bucindolol has serotonin and alpha-adrenoceptor blocking properties. J Cardiovasc Pharmacol. 1985;7 Suppl 7:S67-9. | |||||
REF 87 | 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 88 | Bucindolol: new hopes from reviewing past data.Drugs Today (Barc).2011 May;47(5):347-51. | |||||
REF 89 | Clinical pharmacology of beta 3-adrenoceptors. Br J Clin Pharmacol. 1996 Sep;42(3):291-300. | |||||
REF 90 | 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 91 | Beta-blockers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation. Proc Natl Acad Sci U S A. 2008 Sep 23;105(38):14555-60. | |||||
REF 92 | Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. Br J Pharmacol. 1999 Jun;127(4):895-902. | |||||
REF 93 | Withdrawal syndromes and the cessation of antihypertensive therapy. Arch Intern Med. 1981 Aug;141(9):1125-7. | |||||
REF 94 | Comparison of the beta-adrenoceptor affinity and selectivity of cetamolol, atenolol, betaxolol, and ICI-118,551. J Cardiovasc Pharmacol. 1988 Aug;12(2):208-17. | |||||
REF 95 | (4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. J Med Chem. 2001 Apr 26;44(9):1456-66. | |||||
REF 96 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
REF 97 | 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 98 | Synthesis and beta-adrenergic receptor blocking potency of 1-(substituted amino)-3-(4-indolyloxy)propan-2-ols. J Med Chem. 1986 Aug;29(8):1524-7. | |||||
REF 99 | A vHTS approach for the identification of beta-adrenoceptor ligands. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. | |||||
REF 100 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | |||||
REF 101 | Distribution of beta 1- and beta 2-adrenoceptor subtypes in various mouse tissues. Neurosci Lett. 1993 Sep 17;160(1):96-100. | |||||
REF 102 | Uptake of radioligands by rat heart and lung in vivo: CGP 12177 does and CGP 26505 does not reflect binding to beta-adrenoceptors. Eur J Pharmacol. 1992 Nov 3;222(1):107-12. | |||||
REF 103 | The [(methyloxy)imino]methyl moiety as a bioisoster of aryl. A novel class of completely aliphatic beta-adrenergic receptor antagonists. J Med Chem. 1994 May 13;37(10):1518-25. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.