ReviewBritish journal of pharmacology2010
Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays.
Review in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
What it found
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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.
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Who cites it
51 citing papers in PubMed, 110 citations in OpenAlex.
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Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 2 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
unlabelledCalcium is a key intracellular signal that controls manifold cellular processes over a wide temporal range. The development of calcium-sensitive fluorescent dyes and proteins revolutionized our ability to visualize this important second messenger and its complex signalling characteristics. The subsequent advent of high throughput plate-based fluorescence readers has resulted in the calcium assay becoming the most widely utilized assay system for the characterization of novel receptor ligands. In this review we discuss common approaches to calcium assays, paying particular attention to the potential issues associated with interpretation of receptor pharmacology using this system. Topics covered include dye saturation and forced-coupling of receptors to the calcium pathway, but special consideration is given to the influence of non-equilibrium conditions in this rapid signalling system. Modelling the calcium transient in a kinetic mode allows the influence of ligand kinetics, receptor reserve and read time to be explored. This demonstrates that observed ligand pharmacology at very early time points can be quite different to that determined after longer incubations, even resulting in reversal of agonist potency orders that may be misinterpreted as agonist biased signalling. It also shows that estimates of antagonist affinity, whether by Schild analysis or inhibition curves, are similarly affected by hemi-equilibrium conditions. Finally we end with a discussion on practical approaches to accurately estimate the affinity of insurmountable antagonists using calcium assays. LINKED ARTICLES: This article is part of a themed section on Analytical Receptor Pharmacology in Drug Discovery. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2010.161.issue-6.
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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.