Determination of the pharmacokinetics and oral bioavailability of salicylamine, a potent γ-ketoaldehyde scavenger, by LC/MS/MS

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Abstract

Levels of reactive γ-ketoaldehydes derived from arachidonate increase in diseases associated with inflammation and oxidative injury. To assess the biological importance of these γ-ketoaldehydes, we previously identified salicylamine as an effective γ-ketoaldehyde scavenger in vitro and in cells. To determine if salicylamine could be administered in vivo, we developed an LC/MS/MS assay to measure salicylamine in plasma and tissues. In mice, half-life (t1/2) was 62 minutes. Drinking water supplementation (1-10 g/L) generated tissue concentrations (10-500 μM) within the range previously shown to inhibit γ-ketoaldehydes in cells. Therefore, oral administration of salicylamine can be used to assess the contribution of γ-ketoaldehydes in animal models of disease. © 2010 by the authors licensee Molecular Diversity Preservation International, Basel, Switzerland.

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Zagol-Ikapitte, I., Matafonova, E., Amarnath, V., Bodine, C. L., Boutaud, O., Tirona, R. G., … Davies, S. S. (2010). Determination of the pharmacokinetics and oral bioavailability of salicylamine, a potent γ-ketoaldehyde scavenger, by LC/MS/MS. Pharmaceutics, 2(1), 18–29. https://doi.org/10.3390/pharmaceutics2010018

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