The pharmacological profile of a new, safe, and effective hydrogen sulfide (H2S)-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 H2S 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 H2S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.
Sparatore, A., Perrino, E., Tazzari, V., Giustarini, D., Rossi, R., Rossoni, G., et al. (2009). Pharmacological profile of a novel H(2)S-releasing aspirin. FREE RADICAL BIOLOGY & MEDICINE, 46(5), 586-592 [10.1016/j.freeradbiomed.2008.11.013].
Pharmacological profile of a novel H(2)S-releasing aspirin
GIUSTARINI D;ROSSI, RANIERI;
2009-01-01
Abstract
The pharmacological profile of a new, safe, and effective hydrogen sulfide (H2S)-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 H2S 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 H2S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.
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https://hdl.handle.net/11365/412278