Comparison of filtration and equilibrium dialysis methods for [3H]imipramine binding to human platelets |
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| Authors: | Nelson Lui Richard R. Almon William J. Jusko |
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| Affiliation: | 1. Department of Pharmaceutics, State University of New York at Buffalo, Buffalo, New York 14260 USA;2. Department of Biological Sciences, State University of New York at Buffalo, Buffalo, New York 14260 USA |
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| Abstract: | Receptor binding of imipramine in human platelets was assessed by filtration through glassfiber filters and by equilibrium dialysis. Both methods yield drug-receptor dissociation constants of similar magnitude (10?9m) to literature values. However, the density of binding sites (Bmax) was fivefold lower by filtration (473 ± 92 fmol/mg protein) compared to equilibrium dialysis (2652 ± 765 fmol/mg protein). Dialysis allows direct assessment of free imipramine and avoids drug loss during the separation step of the filtration assay. Additional advantages were found for computer nonlinear regression analysis of untransformed data to eliminate errors owing to linear transformation in the Scatchard analysis and for simultaneous quantitation of nonspecific and total drug binding. |
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| Keywords: | imipramine equilibrium dialysis filtration receptor binding platelets computer analysis |
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