Determine equilibrium dissociation constant of drug-membrane receptor affinity using the cell membrane chromatography relative standard method

Abstract

The equilibrium dissociation constant (K_D) of drug-membrane receptor affinity is the basic parameter that reflects the strength of interaction. The cell membrane chromatography (CMC) method is an effective technique to study the characteristics of drug-membrane receptor affinity. In this study, the K_D value of CMC relative standard method for the determination of drug-membrane receptor affinity was established to analyze the relative K_D values of drugs binding to the membrane receptors (Epidermal growth factor receptor and angiotensin II receptor). The K_D values obtained by the CMC relative standard method had a strong correlation with those obtained by the frontal analysis method. Additionally, the K_D values obtained by CMC relative standard method correlated with pharmacological activity of the drug being evaluated. The CMC relative standard method is a convenient and effective method to evaluate drug-membrane receptor affinity.

Keywords: Cell membrane chromatography; Drug-membrane receptor affinity; Equilibrium dissociation constant; Relative standard method.