The aim of this work was to develop lead pharmacodynamic hybrids, NO-sartans, possessing the characteristics of a typical AT1-antagonist and of a "slow NO donor", by adding NO-donor side chains to losartan. These new compounds, 2a and 2b, displayed vasorelaxing effects, due to the release of NO, and antagonized the vasocontractile effects of angiotensin II, with potency values similar to that of losartan. In vivo, the antihypertensive effects of 2a were similar to those of losartan and captopril.

NO-Sartans: A New Class of Pharmacodynamic Hybrids as Cardiovascular Drugs

BRESCHI, MARIA CRISTINA;CALDERONE, VINCENZO;DIGIACOMO, MARIA;MARTELLI, ALMA;MINUTOLO, FILIPPO;RAPPOSELLI, SIMONA;
2004

Abstract

The aim of this work was to develop lead pharmacodynamic hybrids, NO-sartans, possessing the characteristics of a typical AT1-antagonist and of a "slow NO donor", by adding NO-donor side chains to losartan. These new compounds, 2a and 2b, displayed vasorelaxing effects, due to the release of NO, and antagonized the vasocontractile effects of angiotensin II, with potency values similar to that of losartan. In vivo, the antihypertensive effects of 2a were similar to those of losartan and captopril.
Breschi, MARIA CRISTINA; Calderone, Vincenzo; Digiacomo, Maria; Martelli, Alma; Martinotti, E; Minutolo, Filippo; Rapposelli, Simona; Balsamo, A.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/184511
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