ArticleBritish journal of pharmacology2018
A two-state model for the kinetics of competitive radioligand binding.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed.
- Comparative Real-Time Kinetics of Ligand-Receptor Interactions Using Immobilization-Based Sensing Readouts.Analytical chemistry · 2026Article
- Distinct In Vitro Binding Profile of the Somatostatin Receptor Subtype 2 Antagonist [Pharmaceuticals (Basel, Switzerland) · 2021Article
- Cloning and characterization of the rat Slo3 (KBritish journal of pharmacology · 2020Article
- Considerations for improved performance of competition association assays analysed with the Motulsky-Mahan's "kinetics of competitive binding" model.British journal of pharmacology · 2019Article
- Drug Discovery on Natural Products: From Ion Channels to nAChRs, from Nature to Libraries, from Analytics to Assays.SLAS discovery : advancing life sciences R & D · 2019Review
- A two-state model for the kinetics of competitive radioligand binding.British journal of pharmacology · 2018Article
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Authors and funding
8 authors.
Funding
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Abstract
background and purposeLigand-receptor binding kinetics is receiving increasing attention in the drug research community. The Motulsky and Mahan model, a one-state model, offers a method for measuring the binding kinetics of an unlabelled ligand, with the assumption that the labelled ligand has no preference while binding to distinct states or conformations of a drug target. As such, the one-state model is not applicable if the radioligand displays biphasic binding kinetics to the receptor. EXPERIMENTAL APPROACH: We extended the Motulsky and Mahan model to a two-state model, in which the kinetics of the unlabelled competitor binding to different receptor states (R KEY
resultsThe kinetic rate constants of unlabelled NECA were comparable with the results of kinetic radioligand binding assays in which [
conclusionThe two-state model is sufficient to analyse the binding kinetics of an unlabelled ligand, when a radioligand shows biphasic association characteristics. We expect this two-state model to have general applicability for other targets as well.
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