title: NO-sartans: a new class of pharmacodynamic hybrids as cardiovascular drugs.
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.
authors.affiliation: Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Maria C
authors.initials: MC
authors.lastname: Breschi
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Calderone
authors.forename: Maria
authors.initials: M
authors.lastname: Digiacomo
authors.forename: Alma
authors.initials: A
authors.lastname: Martelli
authors.forename: Enrica
authors.initials: E
authors.lastname: Martinotti
authors.forename: Filippo
authors.initials: F
authors.lastname: Minutolo
authors.forename: Simona
authors.initials: S
authors.lastname: Rapposelli
authors.forename: Aldo
authors.initials: A
authors.lastname: Balsamo
mesh_terms: D047228:Angiotensin II Type 1 Receptor Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D019808:Losartan / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011918:Rats, Inbred SHR; D013329:Structure-Activity Relationship; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D047228:Angiotensin II Type 1 Receptor Blockers; D000959:Antihypertensive Agents; D014665:Vasodilator Agents; D019808:Losartan