ArticleBritish journal of pharmacology2002
Comparison of the affinity of beta-blockers for two states of the beta 1-adrenoceptor in ferret ventricular myocardium.
Article in British journal of pharmacology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 53 citations in OpenAlex.
- Predicting compounds that interact with the 2 known agonist-induced conformations of the human β1-adrenoceptor.Molecular pharmacology · 2025Article
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- Beta-blockers in cardiac arrhythmias-Clinical pharmacologist's point of view.Frontiers in pharmacology · 2022Review
- Bisoprolol protects myocardium cells against ischemia/reperfusion injury by attenuating unfolded protein response in rats.Scientific reports · 2017Article
- Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the humanPharmacology research & perspectives · 2016Article
- Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2015Article
- Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.British journal of pharmacology · 2014Article
- MH-3: evidence for non-competitive antagonism towards the low-affinity site of β1-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
- Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human β1-adrenoceptor.Molecular pharmacology · 2014Article
- 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 · 2011Article
- A full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors.PloS one · 2010Article
- Phosphodiesterases PDE3 and PDE4 jointly control the inotropic effects but not chronotropic effects of (-)-CGP12177 despite PDE4-evoked sinoatrial bradycardia in rat atrium.Naunyn-Schmiedeberg's archives of pharmacology · 2009Article
- Atenolol is inferior to metoprolol in improving left ventricular function and preventing ventricular remodeling in dogs with heart failure.Cardiology · 2009Article
- Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells.BMC pharmacology · 2008Article
- A study of antagonist affinities for the human histamine H2 receptor.British journal of pharmacology · 2008Article
- Multiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates.Trends in pharmacological sciences · 2007Review
- Phosphodiesterase PDE3 blunts the positive inotropic and cyclic AMP enhancing effects of CGP12177 but not of noradrenaline in rat ventricle.British journal of pharmacology · 2006Article
- Positive inotropic and lusitropic effects mediated via the low-affinity state of beta1-adrenoceptors in pithed rats.British journal of pharmacology · 2005Article
- Aspartate138 is required for the high-affinity ligand binding site but not for the low-affinity binding site of the beta1-adrenoceptor.Naunyn-Schmiedeberg's archives of pharmacology · 2004Article
- Markedly reduced effects of (-)-isoprenaline but not of (-)-CGP12177 and unchanged affinity of beta-blockers at Gly389-beta1-adrenoceptors compared to Arg389-beta1-adrenoceptors.British journal of pharmacology · 2004Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We compared the potency of 11 clinically available beta-blockers as antagonists of the positive inotropic effects of (-)-isoprenaline and CGP12177 on ferret ventricular myocardium. (-)-CGP12177, (-)-pindolol and (-)-alprenolol were non-conventional partial agonists with intrinsic activity of 0.7, 0.2 and 0.1 respectively. All beta-blockers antagonized in a concentration-dependent and surmountable manner the positive inotropic effects of both (-)-isoprenaline and CGP12177. The potency of each beta-blocker was consistently higher against (-)-isoprenaline than against CGP12177. Two groups of beta-blockers were identified. In one group the difference between the pK(B) values of blockade against (-)-isoprenaline and CGP12177 was 1.1 - 1.6 log units ((-)-alprenolol, (-)-pindolol, (-)-bupranolol, nadolol and carvedilol). In the other group the pK(B) difference was of 2.1 - 3.0 log units ((-)-atenolol, metoprolol, bisoprolol, sotalol, (-)-propranolol and (-)-timolol). The beta-blockers competed with (-)-[(125)I]-cyanopindolol for binding to ventricular beta(1)-adrenoceptors. The binding affinities correlated with the corresponding blocking potencies against (-)-isoprenaline. On average the pK(i) values were 0.5 log units smaller than the pK(B) values against (-)-isoprenaline but 1.6 log units greater than the pK(B) values against CGP12177. In ferret ventricle the effects of (-)-isoprenaline appear to be antagonized by beta-blockers through the state of the beta(1)-adrenoceptor for which (-)-[(125)I]-cyanopindolol and beta-blockers have high affinity. The cardiostimulant effects of CGP12177 appear to be mediated through a low-affinity state of the beta(1)-adrenoceptor for which beta-blockers have low affinity.
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