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Bioorg Med Chem. 2008 Apr 15;16(8):4661-9. doi: 10.1016/j.bmc.2008.02.033. Epub 2008 Feb 14.

The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.

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  • 1Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47906, USA.


The lipophilicity of a set of 5-HT(2A) ligands was determined using immobilized-artificial-membrane chromatography, a method that generates values well correlated with octanol-water partition coefficients. For agonists, a highly significant linear correlation was observed between binding affinity and lipophilicity. For ligands exhibiting partial agonist or antagonist properties, the lipophilicity was consistently higher than would be expected for an agonist of comparable affinity. The results suggest a possible method for distinguishing agonists from antagonists in high-throughput screening when a direct assay for functional activity is either unavailable or impractical.

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