Elucidation of Vasodilation Response and Structure Activity Relationships of N²,N⁴-Disubstituted Quinazoline 2,4-Diamines in a Rat Pulmonary Artery Model.

ABSTRACT: Pulmonary arterial hypertension (PAH) is a rare and progressive disease arising from various etiologies and pathogenesis. PAH decreases life expectancy due to pulmonary vascular remodeling, elevation of mean pulmonary arterial pressure, and ultimately progresses to heart failure. While clinical treatments are available to reduce the associated symptoms, a complete cure has yet to be found. Phosphodiesterase-5 (PDE-5) inhibition has been identified as a possible intervention point in PAH treatment. The functional vasodilation response to N²,N⁴-diamino quinazoline analogues with differing PDE-5 inhibitory activities and varying physicochemical properties were assessed in both endothelium-intact and denuded rat pulmonary arteries to gain greater insight into their mode of action

SUBMITTER: Paracha TU 

PROVIDER: S-EPMC6358775 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature