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Cell Membrane Chromatography Correlated with Functional Assay for Ligand–β-Adrenergic Receptor Affinities

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Abstract

This study was performed to investigate whether the retention factor (k) from cell membrane chromatography (CMC) can be used to assess the affinity of ligands to β-adrenergic receptor (β-AR) and the correlationship between the factor and pharmacoligical effects. The cell membrane of guinea pig myocardium membrane was immobilized on the surface of the silica carrier as the cell membrane stationary phase (CMSP) for the rapid on-line chromatographic evaluation of ligand binding affinity to β-AR. The affinity was also evaluated by functional assay using the same tissues. Correlation analysis was used to assess the correlationship of these two methods. The retention factors in guinea pig myocardium CMSP were: (−)-propranolol (33.9) > (+)-propranolol (27.0) > metopranolol (23.2) > esmolol (17.7) > practolol (13.2) > sotalol (9.56). Compared to the affinity rank orders obtained from functional assay in the same myocardium, there was a positive correlation (r 2 = 0.9729, n = 18, p < 0.0001) between both data sets. These results showed that CMC can be used to evaluate drug–receptor affinities of drug candidates as the functional assays.

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Acknowledgements

This work was funded by the National Natural Science Foundation of China (NO: 30873194 and 30171079).

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Authors and Affiliations

  1. School of Medicine, Xi’an Jiaotong University, Shaanxi, 710061, China

    Aiguo Zeng, Bingxiang Yuan, Fan Zhu, Limei Zhao, Langchong He & Guangde Yang

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  1. Aiguo Zeng
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  2. Bingxiang Yuan
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  3. Fan Zhu
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  4. Limei Zhao
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  5. Langchong He
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  6. Guangde Yang
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Correspondence to Bingxiang Yuan.

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Zeng, A., Yuan, B., Zhu, F. et al. Cell Membrane Chromatography Correlated with Functional Assay for Ligand–β-Adrenergic Receptor Affinities. Chroma 69, 1373–1377 (2009). https://doi.org/10.1365/s10337-009-1045-8

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