ArticleBritish journal of pharmacology2004
Markedly reduced effects of (-)-isoprenaline but not of (-)-CGP12177 and unchanged affinity of beta-blockers at Gly389-beta1-adrenoceptors compared to Arg389-beta1-adrenoceptors.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers, 1 of them a synthesis that pooled it.
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Who cites it
30 citing papers in PubMed, 1 synthesis or guideline pooled it, 58 citations in OpenAlex.
- β1-adrenoceptor gene Arg389Gly polymorphism and essential hypertension risk in general population: a meta-analysis.Molecular biology reports · 2013Pooled it
- A narrative review of research advancements in pharmacogenetics of cardiovascular disease and impact on clinical implications.NPJ genomic medicine · 2025Review
- Altered O-glycosylation of βThe FEBS journal · 2025Article
- Deciphering the Role of Calcium Signaling Pathway-Associated Single Nucleotide Variants in Susceptibility to Hypertension.Journal of clinical laboratory analysis · 2025Article
- Genetic Variants of Adrenoceptors.Handbook of experimental pharmacology · 2024Review
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- β1-adrenergic receptor polymorphisms: a possible genetic predictor of bisoprolol response in acute coronary syndrome.Future science OA · 2023Article
- Heart failure with reduced ejection fraction and atrial fibrillation: a Sub-Saharan African perspective.ESC heart failure · 2023Review
- Adrenergic receptors gene polymorphisms and autonomic nervous control of heart and vascular tone.Physiological research · 2021Review
- Pharmacogenetic factors affecting β-blocker metabolism and response.Expert opinion on drug metabolism & toxicology · 2020Review
- 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
- Interhelical interaction and receptor phosphorylation regulate the activation kinetics of different human β1-adrenoceptor variants.The Journal of biological chemistry · 2015Article
- Modeling the effects of β1-adrenergic receptor blockers and polymorphisms on cardiac myocyte Ca2+ handling.Molecular pharmacology · 2014Article
- Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor.PloS one · 2013Article
- The genomic architecture of sporadic heart failure.Circulation research · 2011Review
- Human atrial β(1L)-adrenoceptor but not β₃-adrenoceptor activation increases force and Ca(2+) current at physiological temperature.British journal of pharmacology · 2011Article
- Functional effects of β₁-adrenoceptor polymorphisms on the hemodynamic response to dobutamine with and without β-blocker administration.Clinical research in cardiology : official journal of the German Cardiac Society · 2011Article
- The Arg16Gly-β(2)-adrenoceptor single nucleotide polymorphism: exercise capacity and survival in patients with end-stage heart failure.Naunyn-Schmiedeberg's archives of pharmacology · 2010Article
- RAAS and adrenergic genes in heart failure: Function, predisposition and survival implications.World journal of cardiology · 2010Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Substitution of arginine by glycine at position 389, a frequent beta(1)-adrenoceptor polymorphism, reduces adenylyl cyclase stimulation by (-)-isoprenaline. beta(1)-Adrenoceptors mediate the effects of catecholamines and nonconventional partial agonists ((-)-CGP12177) through different sites. We investigated the influence of the 389 polymorphism on beta blocker affinity, as well as on the responses to (-)-isoprenaline and the nonconventional partial agonist (-)-CGP12177 on cyclic AMP levels in CHO cells expressing recombinant Arg389-beta(1)-adrenoceptors (101 fmol mg(-1) protein) or Gly389-beta(1)-adrenoceptors (94 fmol mg(-1)). 2. The affinity of beta-blockers and partial agonists, estimated from competition binding with (-)-[(125)I]-cyanopindolol, was not different for Arg389-beta(1)-adrenoceptors and Gly389-beta(1)-adrenoceptors. 3. The maximum cAMP increases by (-)-isoprenaline and (-)-CGP12177 at Gly389-beta(1)-adrenoceptors were reduced by 97 and 46%, but the potencies enhanced 2 and 0.5 log units, respectively, compared to Arg389-beta(1)-adrenoceptors. The intrinsic activity of (-)-CGP12177 with respect to the (-)-isoprenaline was 0.057 at Arg389-beta(1)-adrenoceptors and 1.05 at Gly389-beta(1)-adrenoceptors. 4. We confirm in intact CHO cells that responses to (-)-isoprenaline are markedly reduced at Gly389-beta(1)-adrenoceptors compared to Arg389-beta(1)-adrenoceptors. However, the 389 polymorphism reduces considerably less the agonist responses to (-)-CGP12177, indicating that coupling to G(s) protein is different for beta(1)-adrenoceptors activated by catecholamines than for receptors activated by nonconventional partial agonists. The affinity of beta-blockers is conserved across the Arg389Gly polymorphism.
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Registered trials
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