The pharmacological profile of a new, safe, and effective hydrogen sulfide (H(2)S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H(2)S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H(2)S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.
Pharmacological profile of a novel H2S-releasing aspirin / A. Sparatore, E. Perrino, V. Tazzari, D. Giustarini, R. Rossi, G. Rossoni, K. Erdmann, H. Schröder, P. Del Soldato. - In: FREE RADICAL BIOLOGY & MEDICINE. - ISSN 0891-5849. - 46:5(2009 Mar 01), pp. 586-592. [10.1016/j.freeradbiomed.2008.11.013]
Pharmacological profile of a novel H2S-releasing aspirin
A. Sparatore;E. Perrino;V. Tazzari;G. Rossoni;
2009
Abstract
The pharmacological profile of a new, safe, and effective hydrogen sulfide (H(2)S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H(2)S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H(2)S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.
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