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The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptors
Article first published online: 29 JAN 2009
DOI: 10.1038/sj.bjp.0706048
2005 British Pharmacological Society
1476-5381/asset/cover.gif?v=1&s=f56f5a76559ff1cebf2b6e329fe028f1e9e0f463 "British Journal of Pharmacology")
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Baker, J. G. (2005), The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptors. British Journal of Pharmacology, 144: 317–322. doi: 10.1038/sj.bjp.0706048
Publication History
- Issue published online: 29 JAN 2009
- Article first published online: 29 JAN 2009
- (Received August 2, 2004, Revised October 5, 2004, Accepted October 12, 2004)
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- 1, , , , , , , , , , , , Biophysical Fragment Screening of the β1-Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design, Journal of Medicinal Chemistry, 2013, 56, 9, 3446
- 2, , , Cardio-Selective Beta-Blocker: Pharmacological Evidence and Their Influence on Exercise Capacity, Cardiovascular Therapeutics, 2013, 31, 2Direct Link:
- 3, , , , , , , , , , Different β-adrenoceptor subtypes coupling to cAMP or NO/cGMP pathways: implications in the relaxant response of rat conductance and resistance vessels, British Journal of Pharmacology, 2013, 169, 2Direct Link:
- 4, , , , , Dose effects of butoxamine, a selective β2-adrenoceptor antagonist, on bone metabolism in spontaneously hypertensive rat, European Journal of Pharmacology, 2013, 701, 1-3, 7
- 5, , Emerging opportunities for allosteric modulation of G-protein coupled receptors, Biochemical Pharmacology, 2013, 85, 2, 153
- 6, , , , , , , , , , Improved survival outcomes with the incidental use of beta-blockers among patients with non-small-cell lung cancer treated with definitive radiation therapy, Annals of Oncology, 2013, 24, 5, 1312
- 7, , , Pathophysiological relevance of the cardiac β2-adrenergic receptor and its potential as a therapeutic target to improve cardiac function, European Journal of Pharmacology, 2013, 698, 1-3, 39
- 8, , , , , Propranolol-induced relaxation in the rat basilar artery, Vascular Pharmacology, 2013, 58, 4, 307
- 9, , , , , , , Synergistic, but not separate, stimulation of accumbal β1- and β2-adrenoceptors alters the accumbal dopamine efflux in freely moving rats, European Journal of Pharmacology, 2013,
- 10, , , , , , Synthesis and in Vitro and in Vivo Characterization of Highly β1-Selective β-Adrenoceptor Partial Agonists, Journal of Medicinal Chemistry, 2013, 130510162633002
- 11, , , β3-Adrenoceptors: a drug target in ophthalmology?, Naunyn-Schmiedeberg's Archives of Pharmacology, 2013, 386, 4, 265
- 12, , , , , G Protein Coupled Receptors - Modeling, Activation, Interactions and Virtual Screening, 2013,
- 13, , , , , , 5-HT induces temporomandibular joint nociception in rats through the local release of inflammatory mediators and activation of local β adrenoceptors, Pharmacology Biochemistry and Behavior, 2012, 102, 3, 458
- 14, , , , , Biased Signaling Pathways in 2-Adrenergic Receptor Characterized by 19F-NMR, Science, 2012, 335, 6072, 1106
- 15, , , , , , , Cell-based and in-silico studies on the high intrinsic activity of two boron-containing salbutamol derivatives at the human β2-adrenoceptor, Bioorganic & Medicinal Chemistry, 2012, 20, 2, 933
- 16, , , , , , , , , , , , Chronic treatment in vivo with β-adrenoceptor agonists induces dysfunction of airway β2-adrenoceptors and exacerbates lung inflammation in mice, British Journal of Pharmacology, 2012, 165, 7Direct Link:
- 17, , , Comparison of Dynamics of Extracellular Accesses to the β1 and β2 Adrenoceptors Binding Sites Uncovers the Potential of Kinetic Basis of Antagonist Selectivity, Chemical Biology & Drug Design, 2012, 80, 2Direct Link:
- 18, , , Effects of hydrocortisone on acute β-adrenoceptor blocker and histamine induced bronchoconstriction, British Journal of Clinical Pharmacology, 2012, 73, 5Direct Link:
- 19, , , , , , , , Efficacy of the β2-adrenergic receptor is determined by conformational equilibrium in the transmembrane region, Nature Communications, 2012, 3, 1045
- 20, , , , , , , Functional investigation of β-adrenoceptors in human isolated detrusor focusing on the novel selective β3-adrenoceptor agonist KUC-7322, Naunyn-Schmiedeberg's Archives of Pharmacology, 2012, 385, 8, 759
- 21, , , , , Heart Rate-Lowering Efficacy and Respiratory Safety of Ivabradine in Patients with Obstructive Airway Disease, American Journal Cardiovascular Drugs, 2012, 12, 3, 179
- 22, , , High-Throughput Analysis of Ligand-Induced Internalization of β2-Adrenoceptors Using the Coiled-Coil Tag–Probe Method, Analytical Chemistry, 2012, 84, 3, 1754
- 23, , , , , , , , , , , Norepinephrine suppresses IFN-γ and TNF-α production by murine intestinal intraepithelial lymphocytes via the β1 adrenoceptor, Journal of Neuroimmunology, 2012, 245, 1-2, 66
- 24, , Theoretical study on some non-selective beta-adrenergic antagonists and correlation to their biologically active configurations, Medicinal Chemistry Research, 2012, 21, 9, 2571
- 25, , , Use of beta-blockers for the treatment of cardiac arrest due to ventricular fibrillation/pulseless ventricular tachycardia: A systematic review, Resuscitation, 2012, 83, 6, 674
- 26, , , α- and β-Adrenergic Receptors Differentially Modulate the Emission of Spontaneous and Amphetamine-Induced 50-kHz Ultrasonic Vocalizations in Adult Rats, Neuropsychopharmacology, 2012, 37, 3, 808
- 27, , , , , , , β-adrenergic-blocking drugs and melanoma: current state of the art, Expert Review of Anticancer Therapy, 2012, 12, 11, 1461
- 28, , , , , β2-adrenoceptors and muscarinic receptors mediate opposing effects on endothelin-1 expression in human lung fibroblasts, European Journal of Pharmacology, 2012, 691, 1-3, 218
- 29, , , , , , , , , , , , , , , A stress response pathway regulates DNA damage through β2-adrenoreceptors and β-arrestin-1, Nature, 2011, 477, 7364, 349
- 30, , , Are there functional β3-adrenoceptors in the human heart?, British Journal of Pharmacology, 2011, 162, 4Direct Link:
- 31, , , Desirable properties of β3-adrenoceptor agonists: Implications for the selection of drug development candidates, European Journal of Pharmacology, 2011, 657, 1-3, 1
- 32, , , , Effects of β-adrenoceptor antagonists on anaphylactic hypotension in conscious rats, European Journal of Pharmacology, 2011, 650, 1, 303
- 33, , , Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling, Trends in Pharmacological Sciences, 2011, 32, 4, 227
- 34, , , , , , , , GPCRs regulate the assembly of a multienzyme complex for purine biosynthesis, Nature Chemical Biology, 2011, 7, 12, 909
- 35, , , , Homology model and docking studies on porcine β2 adrenoceptor: description of two binding sites, Journal of Molecular Modeling, 2011, 17, 10, 2525
- 36, , , , , Human atrial β1L-adrenoceptor but not β3-adrenoceptor activation increases force and Ca2+ current at physiological temperature, British Journal of Pharmacology, 2011, 162, 4Direct Link:
- 37, , , , , , , Ligand-Dependent Perturbation of the Conformational Ensemble for the GPCR β2 Adrenergic Receptor Revealed by HDX, Structure, 2011, 19, 10, 1424
- 38, , , , , Pulmonary Vasoconstrictive and Bronchoconstrictive Responses to Anaphylaxis Are Weakened via β2-adrenoceptor Activation by Endogenous Epinephrine in Anesthetized Rats, Anesthesiology, 2011, 114, 3, 614
- 39, , , , , , , Synthesis and Characterization of High-Affinity 4,4-Difluoro-4-bora-3a,4a-diaza-s-indacene-Labeled Fluorescent Ligands for Human β-Adrenoceptors, Journal of Medicinal Chemistry, 2011, 54, 19, 6874
- 40, , , , , , The design, synthesis and pharmacological characterization of novel β2-adrenoceptor antagonists, British Journal of Pharmacology, 2011, 164, 2Direct Link:
- 41, The development of label-free cellular assays for drug discovery, Expert Opinion on Drug Discovery, 2011, 6, 12, 1285
- 42, , , The effects of acute and chronic nadolol treatment on β2AR signaling in HEK293 cells, Naunyn-Schmiedeberg's Archives of Pharmacology, 2011, 383, 2, 209
- 43, , , , The increase in rat ventricular automaticity induced by salbutamol is mediated through β1- but not β2-adrenoceptors: Role of phosphodiesterases, Life Sciences, 2011, 88, 25-26, 1095
- 44, , , The pharmacological effects of the thermostabilising (m23) mutations and intra and extracellular (β36) deletions essential for crystallisation of the turkey β-adrenoceptor, Naunyn-Schmiedeberg's Archives of Pharmacology, 2011, 384, 1, 71
- 45, , , , , , , , , , , The β2-subtype of adrenoceptors mediates inhibition of pro-fibrotic events in human lung fibroblasts, Naunyn-Schmiedeberg's Archives of Pharmacology, 2011, 384, 2, 133
- 46, , , , β-Adrenoceptor agonist effects in experimental models of bladder dysfunction, Pharmacology & Therapeutics, 2011, 131, 1, 40
- 47, , , , , , , , , , A vHTS approach for the identification of β-adrenoceptor ligands, Bioorganic & Medicinal Chemistry Letters, 2010, 20, 11, 3399
- 48, , , , , , , An efficient asymmetric synthesis of the potent β-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity, Chemical Communications, 2010, 46, 22, 3953
- 49, , , Analysis of hydrophobic interactions of antagonists with the beta2-adrenergic receptor, SAR and QSAR in Environmental Research, 2010, 21, 1-2, 37
- 50, , , , Beta 3-adrenoreceptor regulation of nitric oxide in the cardiovascular system, Journal of Molecular and Cellular Cardiology, 2010, 48, 6, 1088
- You have free access to this content51, , , , , Cardio-selective and non-selective beta-blockers in chronic obstructive pulmonary disease: effects on bronchodilator response and exercise, Internal Medicine Journal, 2010, 40, 3Direct Link:
- 52, , Comparative 3D QSAR study on β1-, β2-, and β3-adrenoceptor agonists, Medicinal Chemistry Research, 2010, 19, 9, 1121
- 53, , , , Docking studies on a refined human β2 adrenoceptor model yield theoretical affinity values in function with experimental values for R-ligands, but not for S-antagonists, Journal of Molecular Modeling, 2010, 16, 3, 401
- 54, , , , , , , , From the Cover: Ghrelin secretion stimulated by 1-adrenergic receptors in cultured ghrelinoma cells and in fasted mice, Proceedings of the National Academy of Sciences, 2010, 107, 36, 15868
- 55, , , Function of cardiac β1- and β2-adrenoceptors of newborn piglets: Role of phosphodiesterases PDE3 and PDE4, European Journal of Pharmacology, 2010, 638, 1-3, 99
- 56, , , , , Lateral Paracapsular GABAergic Synapses in the Basolateral Amygdala Contribute to the Anxiolytic Effects of β3 Adrenoceptor Activation, Neuropsychopharmacology, 2010, 35, 9, 1886
- 57, , , , , , , , , , , , , , , , Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor, Nature, 2010, 463, 7277, 108
- You have free access to this content58, , Mapping the Druggable Allosteric Space of G-Protein Coupled Receptors: a Fragment-Based Molecular Dynamics Approach, Chemical Biology & Drug Design, 2010, 76, 3Direct Link:
- 59, The selectivity of β-adrenoceptor agonists at human β1-, β2- and β3-adrenoceptors, British Journal of Pharmacology, 2010, 160, 5Direct Link:
- 60, , , , , , , Analysis of full and partial agonists binding to β2-adrenergic receptor suggests a role of transmembrane helix V in agonist-specific conformational changes, Journal of Molecular Recognition, 2009, 22, 4Direct Link:
- 61, , , , , , , , , , , , , Metoprolol Reduces Cerebral Tissue Oxygen Tension after Acute Hemodilution in Rats, Anesthesiology, 2009, 111, 5, 988
- 62, , , , , , , , , , One-Year Renal and Cardiac Effects of Bisoprolol versus Losartan in Recently Diagnosed Hypertensive Patients, Clinical Drug Investigation, 2009, 29, 9, 591
- 63, , , , , , Pharmacological evaluation of ocular β-adrenoceptors in rabbit by tissue segment binding method, Life Sciences, 2009, 84, 5-6, 181
- 64, , , Phosphodiesterases inhibition unmask a positive inotropic effect mediated by β2-adrenoceptors in rat ventricular myocardium, European Journal of Pharmacology, 2009, 607, 1-3, 151
- 65, , , The structure and function of G-protein-coupled receptors, Nature, 2009, 459, 7245, 356
- 66, , Think the impossible: β-blockers for treating asthma, Clinical Science, 2009, 118, 2, 115
- 67, , , , , , , , Changes in β2-adrenoceptor and other signaling proteins produced by chronic administration of ‘β-blockers’ in a murine asthma model, Pulmonary Pharmacology & Therapeutics, 2008, 21, 1, 115
- 68, , , , , Comparison of the binding affinity of CGP-12177A at recombinant rat α1D-adrenoceptors expressed in BHK-21 cell membranes and α1-adrenoceptors present in rat cerebral cortex membranes, European Journal of Pharmacology, 2008, 590, 1-3, 303
- 69, Different Pharmacological Properties of Two Enantiomers in a Unique β-Blocker, Nebivolol, Cardiovascular Therapeutics, 2008, 26, 2Direct Link:
- 70, , Identification of potent agonists acting at an endogenous atypical β3-adrenoceptor state that modulate lipolysis in rodent fat cells, European Journal of Pharmacology, 2008, 580, 1-2, 55
- 71, , , , , , , , Low dose beta-blocker prevents ovariectomy-induced bone loss in rats without affecting heart functions, Journal of Cellular Physiology, 2008, 217, 3Direct Link:
- 72, , , , , Role of β1-, β2-, and β3-adrenoceptors in contractile hypersensitivity in a model of small bowel transplantation, Surgery, 2008, 143, 1, 94
- 73, , , , , Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and β-adrenoceptors, Naunyn-Schmiedeberg's Archives of Pharmacology, 2008, 377, 4-6, 449
- 74, , , , , , , , , Structure of a β1-adrenergic G-protein-coupled receptor, Nature, 2008, 454, 7203, 486
- 75, , The low-affinity site of the β1-adrenoceptor and its relevance to cardiovascular pharmacology, Pharmacology & Therapeutics, 2008, 118, 3, 303
- 76, , , Use of the X-ray structure of the β2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds, Bioorganic & Medicinal Chemistry Letters, 2008, 18, 20, 5391
- 77, , , , , , , , , , , , , , , , , A novel transdermal patch incorporating isosorbide dinitrate with bisoprolol: In vitro and in vivo characterization, International Journal of Pharmaceutics, 2007, 337, 1-2, 88
- 78, , , Diagnostic and Therapeutic Challenges in Patients With Coexistent Chronic Obstructive Pulmonary Disease and Chronic Heart Failure, Journal of the American College of Cardiology, 2007, 49, 2, 171
- 79, , , Down-regulation of β1-adrenoceptors gene expression by short interfering RNA impairs the memory retrieval in the basolateral amygdala of rats, Neuroscience Letters, 2007, 428, 2-3, 77
- 80, , , , , Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of α1- and β1-adrenoceptors, British Journal of Pharmacology, 2007, 150, 7Direct Link:
- 81, , , , Getting to the heart of asthma: Can “β blockers” be useful to treat asthma?, Pharmacology & Therapeutics, 2007, 115, 3, 360
- 82, Interleukin 13 and the β-adrenergic blockade theory of asthma revisited 40 years later, Annals of Allergy, Asthma & Immunology, 2007, 99, 3, 215
- 83, , , , , , , , , , , , Medium-term effects of bisoprolol administration on renal hemodynamics and function in mild to moderate essential hypertension, Advances in Therapy, 2007, 24, 6, 1260
- 84, , Multiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates, Trends in Pharmacological Sciences, 2007, 28, 8, 374
- 85, , , , The effects and selectivity of β-adrenoceptor agonists in rat myometrium and urinary bladder, European Journal of Pharmacology, 2007, 573, 1-3, 184
- 86, , , , , , , The Influence of prolonged β-blockers treatment on male rabbit's sexual behavior and penile microcirculation, International Journal of Impotence Research, 2007, 19, 1, 49
- 87, , Tools to study β3-adrenoceptors, Naunyn-Schmiedeberg's Archives of Pharmacology, 2007, 374, 5-6, 385
- 88, , , , β2-ADRENOCEPTOR POLYMORPHISMS AND OBSTRUCTIVE AIRWAY DISEASES: IMPORTANT ISSUES OF STUDY DESIGN, Clinical and Experimental Pharmacology and Physiology, 2007, 34, 10Direct Link:
- 89, , , , , Agonist effects of zinterol at the mouse and human β3-adrenoceptor, Naunyn-Schmiedeberg's Archives of Pharmacology, 2006, 373, 2, 158
- 90, , , Cardiac implications for the use of β2-adrenoceptor agonists for the management of muscle wasting, British Journal of Pharmacology, 2006, 147, 6Direct Link:
- 91, , , , , , , , , , , Carvedilol-induced antagonism of angiotensin II: a matter of α1-adrenoceptor blockade, Journal of Hypertension, 2006, 24, 7, 1355
- 92, , , , Comparison of three radioligands for the labelling of human β-adrenoceptor subtypes, Naunyn-Schmiedeberg's Archives of Pharmacology, 2006, 374, 2, 99
- 93, , , Effects of gender, age and hypertension on β-adrenergic receptor function in rat urinary bladder, Naunyn-Schmiedeberg's Archives of Pharmacology, 2006, 373, 4, 300
- 94, , , , , , Zur Funktion des β3-Adrenozeptors am Herzen: Signaltransduktion, inotroper Effekt und therapeutischer Ausblick, Wiener Medizinische Wochenschrift, 2006, 156, 15-16, 451
- 95, , α1-, α2- and β-adrenoceptors in the urinary bladder, urethra and prostate, British Journal of Pharmacology, 2006, 147, S2Direct Link:
- 96, , β-Rezeptorenblocker bei kardiovaskulären Erkrankungen, Clinical Research in Cardiology Supplements, 2006, 1, 1, 43
- 97, , , β3-Adrenoceptor agonist stimulation of the Na+,K+-pump in rat skeletal muscle is mediated by β2- rather than β3-adrenoceptors, British Journal of Pharmacology, 2006, 149, 6Direct Link:
- 98, , , , , , , Direct demonstration of β1- and evidence against β2- and β3-adrenoceptors, in smooth muscle cells of rat small mesenteric arteries, British Journal of Pharmacology, 2005, 146, 5Direct Link:
- 99, , , , Emerging concepts and therapeutic implications of β-adrenergic receptor subtype signaling, Pharmacology & Therapeutics, 2005, 108, 3, 257
- 100, G-protein-coupled receptors: Better beta-blockers, Nature Reviews Drug Discovery, 2005, 4, 5, 371
- 101, , , , , Role of β2-adrenoceptors (ß-AR), but not ß1-, β3-AR and endothelial nitric oxide, in β-AR-mediated relaxation of rat intrapulmonary artery, Naunyn-Schmiedeberg's Archives of Pharmacology, 2005, 372, 1, 14