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
Click to Show/Hide
|
|||||
| 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] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
|
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Calcium signaling pathway | hsa04020 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| cGMP-PKG signaling pathway | hsa04022 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| cAMP signaling pathway | hsa04024 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Adrenergic signaling in cardiomyocytes | hsa04261 | Affiliated Target |
|
| Class: Organismal Systems => Circulatory system | Pathway Hierarchy | ||
| Gap junction | hsa04540 | Affiliated Target |
|
| Class: Cellular Processes => Cellular community - eukaryotes | Pathway Hierarchy | ||
| Regulation of lipolysis in adipocytes | hsa04923 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Renin secretion | hsa04924 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Salivary secretion | hsa04970 | Affiliated Target |
|
| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Click to Show/Hide the Information of Affiliated Human Pathways | |||
| Degree | 3 | Degree centrality | 3.22E-04 | Betweenness centrality | 7.52E-05 |
|---|---|---|---|---|---|
| Closeness centrality | 2.05E-01 | Radiality | 1.36E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 4.40E+01 | Topological coefficient | 3.81E-01 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| 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.