Pharmacological profile of a novel H2S-releasing aspirin |
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| Authors: | Anna Sparatore Elena Perrino Valerio Tazzari Daniela Giustarini Ranieri Rossi Giuseppe Rossoni Kati Erdman Henning Schröder Piero Del Soldato |
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| Institution: | 1. Dipartimento di Farmacia, Università di Pisa, via Bonanno, 6, I-56126 Pisa, Italy;2. Dipartimento di Chimica e Chimica Industriale, Università di Pisa, via Risorgimento, 35, I-56126 Pisa, Italy;2. Department of Pharmacy, National University of Singapore, Singapore;3. Neurobiology Program, Life Science Institute and Department of Pharmacology, National University of Singapore, Singapore |
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| 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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