The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.

PubWeight™: 2.73‹?› | Rank: Top 1%

🔗 View Article (PMC 1576008)

Published in Br J Pharmacol on February 01, 2005

Authors

Jillian G Baker1

Author Affiliations

1: Institute of Cell Signalling, C Floor Medical School, Queen's Medical Centre, University of Nottingham, Nottingham NG7 2UH, UK. jillian.baker@nottingham.ac.uk

Articles citing this

(truncated to the top 100)

Structure of a beta1-adrenergic G-protein-coupled receptor. Nature (2008) 11.97

The structure and function of G-protein-coupled receptors. Nature (2009) 8.08

The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors. Br J Pharmacol (2013) 5.74

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor. Nature (2010) 3.19

Analysis of full and partial agonists binding to beta2-adrenergic receptor suggests a role of transmembrane helix V in agonist-specific conformational changes. J Mol Recognit (2009) 2.05

Alpha1-, alpha2- and beta-adrenoceptors in the urinary bladder, urethra and prostate. Br J Pharmacol (2006) 1.83

The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. Br J Pharmacol (2010) 1.72

Structural Insights into the Dynamic Process of β2-Adrenergic Receptor Signaling. Cell (2015) 1.68

A stress response pathway regulates DNA damage through β2-adrenoreceptors and β-arrestin-1. Nature (2011) 1.64

Discovery of regulators of receptor internalization with high-throughput flow cytometry. Mol Pharmacol (2012) 1.61

Adrenergic modulation of olfactory bulb circuitry affects odor discrimination. Learn Mem (2007) 1.61

Ligand-dependent perturbation of the conformational ensemble for the GPCR β2 adrenergic receptor revealed by HDX. Structure (2011) 1.54

Efficacy of the β₂-adrenergic receptor is determined by conformational equilibrium in the transmembrane region. Nat Commun (2012) 1.40

Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and beta-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol (2007) 1.37

Changes in beta 2-adrenoceptor and other signaling proteins produced by chronic administration of 'beta-blockers' in a murine asthma model. Pulm Pharmacol Ther (2007) 1.30

Multiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates. Trends Pharmacol Sci (2007) 1.29

Stress-mediated increases in systemic and local epinephrine impair skin wound healing: potential new indication for beta blockers. PLoS Med (2009) 1.28

Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. Chem Biol Drug Des (2010) 1.24

Improved survival outcomes with the incidental use of beta-blockers among patients with non-small-cell lung cancer treated with definitive radiation therapy. Ann Oncol (2013) 1.20

Ghrelin secretion stimulated by {beta}1-adrenergic receptors in cultured ghrelinoma cells and in fasted mice. Proc Natl Acad Sci U S A (2010) 1.20

Lateral paracapsular GABAergic synapses in the basolateral amygdala contribute to the anxiolytic effects of beta 3 adrenoceptor activation. Neuropsychopharmacology (2010) 1.18

GPCRs regulate the assembly of a multienzyme complex for purine biosynthesis. Nat Chem Biol (2011) 1.15

Tools to study beta3-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol (2007) 1.14

A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization. BMC Bioinformatics (2010) 1.11

Molecular basis of ligand dissociation in β-adrenergic receptors. PLoS One (2011) 1.06

Chronic treatment in vivo with β-adrenoceptor agonists induces dysfunction of airway β(2) -adrenoceptors and exacerbates lung inflammation in mice. Br J Pharmacol (2012) 1.06

Effects of gender, age and hypertension on beta-adrenergic receptor function in rat urinary bladder. Naunyn Schmiedebergs Arch Pharmacol (2006) 1.03

Impedance responses reveal β₂-adrenergic receptor signaling pluridimensionality and allow classification of ligands with distinct signaling profiles. PLoS One (2012) 1.02

A full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors. PLoS One (2010) 0.99

Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design. J Med Chem (2013) 0.99

Beta 3-adrenoreceptor regulation of nitric oxide in the cardiovascular system. J Mol Cell Cardiol (2010) 0.98

Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling. Trends Pharmacol Sci (2011) 0.97

Direct demonstration of beta1- and evidence against beta2- and beta3-adrenoceptors, in smooth muscle cells of rat small mesenteric arteries. Br J Pharmacol (2005) 0.95

α- and β-Adrenergic receptors differentially modulate the emission of spontaneous and amphetamine-induced 50-kHz ultrasonic vocalizations in adult rats. Neuropsychopharmacology (2011) 0.93

Different β-adrenoceptor subtypes coupling to cAMP or NO/cGMP pathways: implications in the relaxant response of rat conductance and resistance vessels. Br J Pharmacol (2013) 0.92

Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of alpha1- and beta1-adrenoceptors. Br J Pharmacol (2007) 0.92

Comparison of three radioligands for the labelling of human beta-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol (2006) 0.91

Stress-induced cocaine seeking requires a beta-2 adrenergic receptor-regulated pathway from the ventral bed nucleus of the stria terminalis that regulates CRF actions in the ventral tegmental area. J Neurosci (2014) 0.91

Application of BRET to monitor ligand binding to GPCRs. Nat Methods (2015) 0.91

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. J Med Chem (2011) 0.89

Catecholamine stress alters neutrophil trafficking and impairs wound healing by β2-adrenergic receptor-mediated upregulation of IL-6. J Invest Dermatol (2013) 0.88

beta-Adrenergic activation of electrogenic K+ and Cl- secretion in guinea pig distal colonic epithelium proceeds via separate cAMP signaling pathways. Am J Physiol Gastrointest Liver Physiol (2010) 0.88

Full and partial agonists of muscarinic M3 receptors reveal single and oscillatory Ca2+ responses by beta 2-adrenoceptors. J Pharmacol Exp Ther (2009) 0.87

Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism. JAMA Ophthalmol (2013) 0.87

The β2-subtype of adrenoceptors mediates inhibition of pro-fibrotic events in human lung fibroblasts. Naunyn Schmiedebergs Arch Pharmacol (2011) 0.87

Human atrial β(1L)-adrenoceptor but not β₃-adrenoceptor activation increases force and Ca(2+) current at physiological temperature. Br J Pharmacol (2011) 0.86

Beta adrenergic modulation of spontaneous microcontractions and electrical field-stimulated contractions in isolated strips of rat urinary bladder from normal animals and animals with partial bladder outflow obstruction. Naunyn Schmiedebergs Arch Pharmacol (2015) 0.86

Thermodynamics and docking of agonists to the β(2)-adrenoceptor determined using [(3)H](R,R')-4-methoxyfenoterol as the marker ligand. Mol Pharmacol (2012) 0.86

Induction of intracellular calcium concentration by environmental benzo(a)pyrene involves a β2-adrenergic receptor/adenylyl cyclase/Epac-1/inositol 1,4,5-trisphosphate pathway in endothelial cells. J Biol Chem (2011) 0.86

Adrenergic pathway activation enhances brown adipose tissue metabolism: a [¹⁸F]FDG PET/CT study in mice. Nucl Med Biol (2013) 0.86

Norepinephrine enhances the LPS-induced expression of COX-2 and secretion of PGE2 in primary rat microglia. J Neuroinflammation (2010) 0.85

Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses. FASEB J (2011) 0.84

Functional investigation of β-adrenoceptors in human isolated detrusor focusing on the novel selective β3-adrenoceptor agonist KUC-7322. Naunyn Schmiedebergs Arch Pharmacol (2012) 0.83

Effects of hydrocortisone on acute β-adrenoceptor blocker and histamine induced bronchoconstriction. Br J Clin Pharmacol (2012) 0.83

β-Blocker dialyzability and mortality in older patients receiving hemodialysis. J Am Soc Nephrol (2014) 0.83

Do β-adrenoceptor agonists induce homologous or heterologous desensitization in rat urinary bladder? Naunyn Schmiedebergs Arch Pharmacol (2013) 0.83

Total beta-adrenoceptor knockout slows conduction and reduces inducible arrhythmias in the mouse heart. PLoS One (2012) 0.82

The pharmacological effects of the thermostabilising (m23) mutations and intra and extracellular (β36) deletions essential for crystallisation of the turkey β-adrenoceptor. Naunyn Schmiedebergs Arch Pharmacol (2011) 0.82

Role of beta2-adrenoceptors (beta-AR), but not beta1-, beta3-AR and endothelial nitric oxide, in beta-AR-mediated relaxation of rat intrapulmonary artery. Naunyn Schmiedebergs Arch Pharmacol (2005) 0.82

What can crystal structures of aminergic receptors tell us about designing subtype-selective ligands? Pharmacol Rev (2015) 0.82

The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion. FASEB J (2015) 0.81

Agonist effects of zinterol at the mouse and human beta(3)-adrenoceptor. Naunyn Schmiedebergs Arch Pharmacol (2006) 0.81

Inhibition of human melanoma growth by a non-cardioselective β-blocker. J Invest Dermatol (2014) 0.81

Adrenergic Receptors in Individual Ventricular Myocytes: The Beta-1 and Alpha-1B Are in All Cells, the Alpha-1A Is in a Subpopulation, and the Beta-2 and Beta-3 Are Mostly Absent. Circ Res (2017) 0.80

Adrenoceptor activity of muscarinic toxins identified from mamba venoms. Br J Pharmacol (2011) 0.80

Docking studies on a refined human beta(2) adrenoceptor model yield theoretical affinity values in function with experimental values for R-ligands, but not for S-antagonists. J Mol Model (2009) 0.80

The temporal hormesis of drug therapies. Dose Response (2006) 0.80

Are there functional β₃-adrenoceptors in the human heart? Br J Pharmacol (2011) 0.80

A pathway and network review on beta-adrenoceptor signaling and beta blockers in cardiac remodeling. Heart Fail Rev (2014) 0.79

Cardiovascular responses to retigabine in conscious rats--under normotensive and hypertensive conditions. Br J Pharmacol (2013) 0.79

Prostaglandin E2 excitatory effects on rat urinary bladder: a comparison between the β-adrenoceptor modulation of non-voiding activity in vivo and micro-contractile activity in vitro. Naunyn Schmiedebergs Arch Pharmacol (2015) 0.79

Perioperative landiolol administration reduces atrial fibrillation after cardiac surgery: A meta-analysis of randomized controlled trials. Adv Ther (2014) 0.79

Homology model and docking studies on porcine β₂ adrenoceptor: description of two binding sites. J Mol Model (2011) 0.79

Activation of β2-adrenergic receptor by (R,R')-4'-methoxy-1-naphthylfenoterol inhibits proliferation and motility of melanoma cells. Cell Signal (2015) 0.79

The design, synthesis and pharmacological characterization of novel β₂-adrenoceptor antagonists. Br J Pharmacol (2011) 0.78

Quantification of beta adrenergic receptor subtypes in beta-arrestin knockout mouse airways. PLoS One (2015) 0.78

Atenolol is inferior to metoprolol in improving left ventricular function and preventing ventricular remodeling in dogs with heart failure. Cardiology (2008) 0.78

Underuse of β-blockers in heart failure and chronic obstructive pulmonary disease. Heart (2016) 0.78

Comparison of dynamics of extracellular accesses to the β(1) and β(2) adrenoceptors binding sites uncovers the potential of kinetic basis of antagonist selectivity. Chem Biol Drug Des (2012) 0.78

Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists. J Med Chem (2013) 0.78

[On the function of beta3-adrenoceptors in the human heart: signal transduction, inotropic effect and therapeutic prospects]. Wien Med Wochenschr (2006) 0.78

GPCR endocytosis confers uniformity in responses to chemically distinct ligands. Mol Pharmacol (2016) 0.77

Cardiac implications for the use of beta2-adrenoceptor agonists for the management of muscle wasting. Br J Pharmacol (2006) 0.77

β-Adrenergic receptor antagonism in mice: a model for pediatric heart disease. J Appl Physiol (1985) (2013) 0.77

Epinephrine Activation of the β2-Adrenoceptor Is Required for IL-13-Induced Mucin Production in Human Bronchial Epithelial Cells. PLoS One (2015) 0.77

Beta3-adrenoceptor agonist stimulation of the Na+, K+ -pump in rat skeletal muscle is mediated by beta2- rather than beta3-adrenoceptors. Br J Pharmacol (2006) 0.77

Can [I]-Iodocyanopindolol Label β(3)-Adrenoceptors in Rat Urinary Bladder? Front Pharmacol (2010) 0.77

Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor. ACS Med Chem Lett (2013) 0.77

β3 Adrenergic Stimulation Restores Nitric Oxide/Redox Balance and Enhances Endothelial Function in Hyperglycemia. J Am Heart Assoc (2016) 0.76

Dynamic mass redistribution reveals diverging importance of PDZ-ligands for G protein-coupled receptor pharmacodynamics. Pharmacol Res (2016) 0.76

Ozone-Induced Hypertussive Responses in Rabbits and Guinea Pigs. J Pharmacol Exp Ther (2016) 0.76

Beta1-adrenergic receptor-mediated dilation of rat cerebral artery requires Shaker-type KV1 channels on PSD95 scaffold. J Cereb Blood Flow Metab (2015) 0.76

β-Adrenergic Stimulation Induces Histone Deacetylase 5 (HDAC5) Nuclear Accumulation in Cardiomyocytes by B55α-PP2A-Mediated Dephosphorylation. J Am Heart Assoc (2017) 0.75

Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists. Med Chem Res (2009) 0.75

Dual regulation of β2-adrenoceptor messenger RNA expression in human lung fibroblasts by β2-cAMP signaling; delayed upregulated inhibitors oppose a rapid in onset, direct stimulation of gene expression. Naunyn Schmiedebergs Arch Pharmacol (2014) 0.75

Carvedilol induces greater control of β2- than β 1-adrenoceptor-mediated inotropic and lusitropic effects by PDE3, while PDE4 has no effect in human failing myocardium. Naunyn Schmiedebergs Arch Pharmacol (2014) 0.75

Effect of selective β-adrenoceptor blockade and surgical resection of the celiac-superior mesenteric ganglion complex on delayed liquid gastric emptying induced by dipyrone, 4-aminoantipyrine, and antipyrine in rats. Braz J Med Biol Res (2016) 0.75

Probing the stoichiometry of β2-adrenergic receptor phosphorylation by targeted mass spectrometry. J Mol Signal (2014) 0.75

Drug Therapy for Hypertrophic Cardiomypathy: Physiology and Practice. Curr Cardiol Rev (2016) 0.75

Search for β2 adrenergic receptor ligands by virtual screening via grid computing and investigation of binding modes by docking and molecular dynamics simulations. PLoS One (2014) 0.75

Articles cited by this

The Cardiac Insufficiency Bisoprolol Study II (CIBIS-II): a randomised trial. Lancet (1999) 11.26

Comparison of carvedilol and metoprolol on clinical outcomes in patients with chronic heart failure in the Carvedilol Or Metoprolol European Trial (COMET): randomised controlled trial. Lancet (2003) 9.80

Comparison of some properties of pronethalol and propranolol. Br J Pharmacol Chemother (1965) 4.71

A trial of the beta-blocker bucindolol in patients with advanced chronic heart failure. N Engl J Med (2001) 4.07

Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc Natl Acad Sci U S A (2003) 3.75

Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the beta 2-adrenoceptor. Nature (1995) 3.27

Inverse agonist activity of beta-adrenergic antagonists. Mol Pharmacol (1994) 2.22

Adrenergic receptors as models for G protein-coupled receptors. Annu Rev Neurosci (1992) 2.04

Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol (2004) 1.95

Isoproterenol antagonism of cardioselective beta adrenergic receptor blocking agents: a comparative study of human and guinea-pig cardiac and bronchial beta adrenergic receptors. J Pharmacol Exp Ther (1976) 1.74

Agonist and inverse agonist actions of beta-blockers at the human beta 2-adrenoceptor provide evidence for agonist-directed signaling. Mol Pharmacol (2003) 1.67

Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors. Cardiovasc Drugs Ther (1999) 1.60

Agonist actions of "beta-blockers" provide evidence for two agonist activation sites or conformations of the human beta1-adrenoceptor. Mol Pharmacol (2003) 1.52

Meta-analysis of trials comparing beta-blockers, calcium antagonists, and nitrates for stable angina. JAMA (1999) 1.43

Pharmacological characterization of CGP 12177 at the human beta(2)-adrenoceptor. Br J Pharmacol (2002) 1.08

Use of beta-adrenoceptor blocking drugs in hyperthyroidism. Drugs (1984) 1.05

Amplification of cyclic AMP generation reveals agonistic effects of certain beta-adrenergic antagonists. Mol Pharmacol (1990) 1.05

Influence of agonist efficacy and receptor phosphorylation on antagonist affinity measurements: differences between second messenger and reporter gene responses. Mol Pharmacol (2003) 1.02

Allosteric effects of G protein overexpression on the binding of beta-adrenergic ligands with distinct inverse efficacies. Mol Pharmacol (2001) 0.96

Primary drug treatment for glaucoma: beta-blockers versus other medications. Surv Ophthalmol (2002) 0.94

Beta-adrenergic blocking drugs in the treatment of hypertension. Blood Press (2001) 0.94

Adverse reactions with beta-adrenoceptor blocking drugs. An update. Drug Saf (1993) 0.91

The prevention of migraine: a critical review with special emphasis on beta-adrenoceptor blockers. Br J Clin Pharmacol (2001) 0.90

Profile of ligand binding to the porcine beta2-adrenergic receptor. J Anim Sci (2001) 0.85

Beta-blockers in the treatment of neurological and psychiatric disorders. J Clin Hosp Pharm (1981) 0.84

Medical treatment of essential tremor and Parkinson's disease. Geriatrics (1998) 0.84

Beta-blockage therapy and cardiovascular disease. Past, present, and future. Postgrad Med (1988) 0.84