ArticleBritish journal of pharmacology2019
Model-free and kinetic modelling approaches for characterising non-equilibrium pharmacological pathway activity: Internalisation of cannabinoid CB
Article in British journal of pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 25 citations in OpenAlex.
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- Canonical Cannabinoid Receptors.Current topics in behavioral neurosciences · 2026Review
- Insight into the mechanism of action of ORG27569 at the cannabinoid type one receptor utilising a unified mathematical model.Naunyn-Schmiedeberg's archives of pharmacology · 2024Article
- Kinetic insights into agonist-dependent signalling bias at the pro-inflammatory G-protein coupled receptor GPR84.European journal of pharmacology · 2023Article
- Kinetic analysis of endogenous βBritish journal of pharmacology · 2023Article
- SGIP1 in axons prevents internalization of desensitized CB1R and modifies its function.Frontiers in neuroscience · 2023Review
- In Vitro Characterization of 6-Methyl-3-(2-nitro-1-(thiophen-2-yl)ethyl)-2-phenyl-1ACS pharmacology & translational science · 2022Article
- Quantifying the Kinetics of Signaling and Arrestin Recruitment by Nervous System G-Protein Coupled Receptors.Frontiers in cellular neuroscience · 2021Article
- Evaluation of the profiles of CBBritish journal of pharmacology · 2020Article
- Analyzing kinetic signaling data for G-protein-coupled receptors.Scientific reports · 2020Article
- 100 years of modelling ligand-receptor binding and response: A focus on GPCRs.British journal of pharmacology · 2020Review
- Do Toxic Synthetic Cannabinoid Receptor Agonists Have Signature in Vitro Activity Profiles? A Case Study of AMB-FUBINACA.ACS chemical neuroscience · 2019Article
- Model-free and kinetic modelling approaches for characterising non-equilibrium pharmacological pathway activity: Internalisation of cannabinoid CBBritish journal of pharmacology · 2019Article
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeReceptor internalisation is by nature kinetic. Application of a standard equilibrium dose response model to describe the properties of a ligand inducing internalisation, while commonly used, are therefore problematic. Here, we propose two quantitative approaches to address this issue-(a) a model-free method and (b) a kinetic modelling approach-and systematically evaluate the performance of these methods against traditional equilibrium methods to characterise the internalisation profiles of cannabinoid CB EXPERIMENTAL APPROACH: Kinetic internalisation assays were conducted using a concentration series of six CB KEY
resultsRates of receptor internalisation depended on both agonist and concentration. Agonist potencies from snapshot equilibrium analysis increased with stimulation time, and there was no single time point at which internalisation profiles could infer agonist properties in a comparative manner. The model-free method yielded a time-invariant measure of potency/efficacy for internalisation. The kinetic model adequately described the internalisation of CB CONCLUSION AND IMPLICATIONS: Applying equilibrium analysis to a non-equilibrium pathway cannot provide a reliable estimate of agonist potency. Both the model-free and kinetic modelling approaches characterised the internalisation profiles of CB
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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.