ArticleBritish journal of pharmacology2002
Pharmacological characterization of CGP 12177 at the human beta(2)-adrenoceptor.
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 20 papers.
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Who cites it
20 citing papers in PubMed, 44 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
- CRISPR/Cas9-mediated generation and analysis of N terminus polymorphic models of βMolecular therapy. Methods & clinical development · 2021Article
- Carvedilol inhibits EGF-mediated JB6 P+ colony formation through a mechanism independent of adrenoceptors.PloS one · 2019Article
- A monoclonal antibody raised against a thermo-stabilised βBiochemical pharmacology · 2018Article
- A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-AFrontiers in pharmacology · 2017Article
- 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
- Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization.British journal 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
- Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.Biochimica et biophysica acta · 2014Review
- Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay.Chemistry & biology · 2012Article
- Homology model and docking studies on porcine β₂ adrenoceptor: description of two binding sites.Journal of molecular modeling · 2011Article
- A full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors.PloS one · 2010Article
- The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.British journal of pharmacology · 2010Article
- Beta-arrestin scaffolding of phosphatidylinositol 4-phosphate 5-kinase Ialpha promotes agonist-stimulated sequestration of the beta2-adrenergic receptor.The Journal of biological chemistry · 2008Article
- G-protein-coupled receptors: past, present and future.British journal of pharmacology · 2006Article
- The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology · 2005Article
- Overexpression of beta 1-adrenoceptors in adult rat ventricular myocytes enhances CGP 12177A cardiostimulation: implications for 'putative' beta 4-adrenoceptor pharmacology.British journal of pharmacology · 2004Article
- Do fluorescent drugs show you more than you wanted to know?British journal of pharmacology · 2003Article
- Pharmacology and direct visualisation of BODIPY-TMR-CGP: a long-acting fluorescent beta2-adrenoceptor agonist.British journal of pharmacology · 2003Article
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3 authors at 2 institutions in 1 country.
Funding
Abstract
1 It has recently been reported that CGP 12177 can act as an agonist at a novel secondary site within the human beta(1)-adrenoceptor. The aim of this study was to undertake a detailed pharmacological study of the effects of CGP 12177 on the human beta(2)-adrenoceptor. 2 CGP 12177 acted as a potent partial agonist of (3)H-cyclic AMP accumulation (log EC(50)-8.90+/-0.06) and CRE-mediated reporter gene transcription (log EC(50)-9.66+/-0.04) in CHO-K1 cells expressing the human beta(2)-adrenoceptor. These CGP-induced responses were antagonized by the beta(2)-selective antagonist ICI 118551 (apparent log K(D) values of -8.84+/-0.15 and -9.51+/-0.02 for the cyclic AMP and reporter gene responses respectively). 3 CGP 12177 was also able to antagonize both cyclic AMP and reporter gene responses to more efficacious beta(2)-agonists with similar log K(D) values (e.g. -9.57+/-0.15 and -10.04+/-0.096 respectively with salbutamol as agonist). 4 (3)H-CGP 12177 binding to beta(2)-adrenoceptors in intact CHO-beta(2) cells yielded a log K(D) value of -9.84+/-0.06, but indicated that the ligand dissociates very slowly from the receptor (t(1/2) for dissociation=65 min). However, studies with a Green Fluorescent Protein (GFP)-tagged beta(2)-adrenoceptor indicated that CGP 12177 does not stimulate beta(2)-adrenoceptor internalization. 5 This study demonstrates that CGP 12177 is a high affinity partial agonist of both cAMP accumulation and CRE-mediated gene transcription at the human beta(2)-adrenoceptor. It provides no evidence that CGP 12177 can discriminate a secondary site on the beta(2)-adrenoceptor analogous to that observed for the human beta(1)-adrenoceptor. However, despite its very weak actions on cAMP accumulation, the potent agonist effects of CGP 12177 on CRE-mediated gene transcription at the human beta(2)-adrenoceptor, coupled with its long duration of action, offers a potential lead for drug development for the treatment of chronic inflammatory airway diseases.
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