Comparison of determination of drug-muscarinic receptor affinity by cell-membrane chromatography and by radioligand-binding assay with the cerebrum membrane of the rat

This study was performed to determine whether cell-membrane chromatography (CMC) can be used to reflect the selectivity and specificity of interactions between drugs and the muscarinic acetylcholine receptor (mAChR). A cell membrane stationary phase (CMSP) was prepared by immobilizing rat cerebrum cell membrane on the surface of a silica carrier and used for rapid on-line chromatographic evaluation of ligand binding affinity to mAChR. Comparison of the results with affinity rank orders obtained from radioligand-binding assays using the same cerebrum membrane indicated a positive correlation (r(2) = 0.8640, n = 18, P < 0.0001) between the data sets and proved that CMC can be used to evaluate drug-receptor affinity for drug candidates.