Screening of 5-HT1A Receptor Antagonists using Molecularly Imprinted Polymers

J. Am. Chem. Soc. 2007, 129, 1680—1689

Molecular imprinting produces network polymers with recognition sites for imprint molecules. MIPs can serve as crude mimics of native receptors. To evaluate the relationship between MIPs and native receptors, imprinted polymers for WAY-100635, an antagonist of the serotonin (5-HT) receptor subtype 5-HT1A were prepared. The resulting MIP P(WAY) was evaluated as an affinity matrix in the screening of serotonin receptor antagonists with known affinities for the native receptor. Correlations in affinity between the synthetic P(WAY) and native receptor 5-HT1A were found. These findings provide support for the analogy between MIPs and native receptors and their possible use as surrogates.

Relationship between 5-HT1A binding affinity and imprinting factors: (a) 1 mL/min in 7:3 ACN/10 mM KH2PO4 + K2HPO4 (aq, pH 5.8).