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

- CMC relative standard method (CMC-RSM) for determining drug-membrane receptor affinity is established.
- The KD values obtained by CMC-RSM were positively correlated with those obtained by frontal analysis.
- The KD values obtained by CMC-RSM were correlated with pharmacological activity of the drugs.

The equilibrium dissociation constant (KD) 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 KD value of CMC relative standard method for the determination of drug-membrane receptor affinity was established to analyze the relative KD values of drugs binding to the membrane receptors (Epidermal growth factor receptor and angiotensin II receptor). The KD values obtained by the CMC relative standard method had a strong correlation with those obtained by the frontal analysis method. Additionally, the KD 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.