Model-free and kinetic modelling approaches for characterising non-equilibrium pharmacological pathway activity: Internalisation of cannabinoid CB1 receptors.
Xiao ZhuDavid B FinlayMichelle GlassStephen B DuffullPublished in: British journal of pharmacology (2019)
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 CB1 receptor agonists. The kinetic model provides additional advantages as a method to capture changes in receptor number during other functional assays.