ReviewBritish journal of pharmacology2009
Agonist efficacy and receptor desensitization: from partial truths to a fuller picture.
Review in British journal of pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
25 citing papers in PubMed, 61 citations in OpenAlex.
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- Inhaled βBreathe (Sheffield, England) · 2016Article
- Salmeterol Efficacy and Bias in the Activation and Kinase-Mediated Desensitization of β2-Adrenergic Receptors.Molecular pharmacology · 2015Article
- Functional desensitization of the β 2 adrenoceptor is not dependent on agonist efficacy.Pharmacology research & perspectives · 2015Article
- Assessing Gonadotropin Receptor Function by Resonance Energy Transfer-Based Assays.Frontiers in endocrinology · 2015Article
- The role of indacaterol for chronic obstructive pulmonary disease (COPD).Journal of thoracic disease · 2013Article
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- Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists.British journal of pharmacology · 2012Article
- Discovery of 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists.Journal of medicinal chemistry · 2011Article
- β(2) -adrenoceptor agonists: current and future direction.British journal of pharmacology · 2011Review
Corrections and comments
- Comment on
Authors and funding
1 author at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
It has been demonstrated that the degree of agonist-induced desensitization of the beta(2)-adrenoceptor is related to agonist efficacy (strength of signalling), whereby high-efficacy agonists (e.g. formoterol) cause more phosphorylation and internalization of the receptor than low-efficacy agonists (e.g. salmeterol). These early studies, however, used a protocol where agonists were matched for receptor occupancy rather than functional effect. In this issue of the BJP, Duringer and colleagues have extended these studies to compare the ability of agonists to cause desensitization at equi-effective (cAMP signalling) concentrations rather than equal occupancy. Their data and conclusions are quite different from those previously described. After prolonged exposure, all the agonists caused a similar degree of desensitization, whereas a pulse protocol uncovered a greater loss of responsiveness with the low-efficacy ligands. This is consistent with the notion that high-efficacy agonists have 'spare receptors', and are therefore less sensitive to loss of receptors through desensitization. It also reflects experience in the clinic, where both formoterol and salmeterol show a similar early decline in bronchoprotection, after which their effects remain stable. These findings challenge the notion that high-efficacy ligands always cause more functional desensitization.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.