Abstract
Aim:
To study if cell membrane chromatography (CMC) could reflect drug-receptor interaction and evaluate the affinity and competitive binding to muscarinic acetylcholine receptor (mAChR).
Methods:
The cell membrane stationary phase (CMSP) was prepared by immobilizing guinea pig jejunum cell membrane on the surface of a silica carrier, and was used for the rapid on-line chromatographic evaluation of ligand binding affinities to mAChR. The affinity to mAChR was also evaluated from radioligand binding assays (RBA) using the same jejunum membrane preparation.
Results:
The capacity factor (k') profiles in guinea pig jejunum CMSP were: (-)QNB (15.4)>(+)QNB (11.5)>atropine (5.35)>pirenzepine (5.26)>4-DAMP (4.45)>AF-DX116 (4.18)>pilocarpine (3.93)>acetylcholine (1.31). These results compared with the affinity rank orders obtained from radioligand binding assays indicated that there was a positive correlation (r2= 0.8525, P<0.0001) between both data sets.
Conclusion:
The CMC method can be used to evaluate drug-receptor affinities for drug candidates.
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Yuan, Bx., Hou, J., He, Lc. et al. Evaluation of drug-muscarinic receptor affinities using cell membrane chromatography and radioligand binding assay in guinea pig jejunum membrane. Acta Pharmacol Sin 26, 113–116 (2005). https://doi.org/10.1111/j.1745-7254.2005.00015.x
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DOI: https://doi.org/10.1111/j.1745-7254.2005.00015.x
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