AIM To evaluate if
cell membrane chromatography(CMC) can be used to reflect the selectivity and specificity of drug-muscarinic
acetylcholine receptor (mAChR) interaction. METHODS The
cell membrane stationary phase (CMSP) was prepared by immobilizing rat atrium cell membrane on the surface of a silica carrier and used for the rapid on-line chromatographic evaluation of ligand binding affinities to mAChR. RESULTS The capacity factor profiles in rat atrium CMSP were: (-)QNB(11.5)>pirenzepine(4.8)>atropine(4.2)>4-DAMP (3.5)>AF-DX116(2.4)>pilocarpine(1.14)>acetylcholine(1.02). Those results compared with the affinity rank orders obtained from radioligand binding assays using the same atrium tissue indicated there was a positive correlation (r= 0.9, P<0.05) between the both data sets. However, there were some unusual capactity factors. CONCLUSION CMC method can be used to preliminarily evaluate drug-receptor affinities for drug candidates but the accuracy should be validated by traditional radioligand binding assay.