Schild equation

Schild equation

Antagonism

Published in John C. Matthews, Fundamentals of Receptor, Enzyme, and Transport Kinetics, 2017

the Schild equation. Evaluation of the Schild equation requires that the researcher generate a family of Y vs. log [L] curves for a series of I concentrations, such as the one shown in Figure 38. This provides a set of [L’] values that can be plotted as a Schild plot, Figure 39.

The potency of selatogrel, a reversible antagonist of the P2Y12 receptor, is affected by calcium concentration

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Journal Information

Published in Platelets, 2022

Martine Baumann, Benoît Lack, Isabelle Guillaumat, Mark J. Murphy, Markus A. Riederer

Constant concentrations of [3H]-selatogrel (3, 10, 30 and 100 nM, respectively) were incubated with a concentration range of ADP (0.03 μM up to 316 μM). With increasing concentration of ADP, binding of [3H]-selatogrel to the P2Y12 receptor was dose-dependently reduced. In addition, an increase of [3H]-selatogrel concentration resulted in a right-shift of the ADP-inhibition curves toward higher concentrations of ADP (Figure 1c). Analysis of this data with a Schild regression (log [3H]-selatogrel concentration versus log [concentration ratio-1]) [35,36] revealed a linear correlation with a slope of 1.07 (Schild equation: y = 1.07x +8.9) and a correlation factor of 0.95, confirming that [3H]-selatogrel is a competitive antagonist of ADP binding to the P2Y12 receptor (Figure 1d).

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Antagonism

The potency of selatogrel, a reversible antagonist of the P2Y12 receptor, is affected by calcium concentration