Regular ArticleBinding Study of Semotiadil and Levosemotiadil (cas 116476-16-5) with α1-Acid Glycoprotein Using High-Performance Frontal Analysis

Add time:08/13/2019    Source:sciencedirect.com

High-performance frontal analysis (HPFA) was used to investigate the binding properties of human α1-acid glycoprotein (AGP) with semotiadil ((R)-isomer, Ca-channel blocker) and its antipode Levosemotiadil (cas 116476-16-5) ((S)-isomer, Ca- and Na-channel blockers). An on-line HPLC system consisting of a HPFA column, an extraction column, and an analytical HPLC column was used to determine the unbound concentrations of these enantiomers, and the experimental data were subsequently subjected to the Scatchard analyses to estimate their binding parameters. The binding affinity of the (R)-isomer (K = 3.17 × 107 M, n = 0.74) is approximately 1.2 times stronger than that of (S)-isomer (K = 2.59 × 107 M, n = 0.74). An enantioselective competitive binding study indicated that both enantiomers are bound at the same site on AGP molecules.

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