What happens to the log (concentration) vs response curve of a drug in the presence of a competitive antagonist? Assuming that the agonist and the antagonist are in equilibrium with the receptor-binding site, we will observe a parallel shift in the agonist concentration response curve. We can estimate the proportion of agonist and antagonist bound to the receptors by the concentration of the agonist and antagonist and by their affinities for the receptor as follows:

Under the laws of Mass Action, we can derive the following relationship: Continue reading →