Selective SERCA2a activator as a candidate for chronic heart failure therapy.

ABSTRACT:

Background

The sarcoplasmic reticulum (SR) Ca²⁺ ATPase (SERCA2a) depression substantially contributes to diastolic dysfunction in heart failure (HF), suggesting that SERCA2a stimulation may be a mechanism-based HF therapy. Istaroxime is a drug endowed with both a SERCA2a stimulatory activity and a Na⁺/K⁺ pump inhibitory activity for acute HF treatment. Its main metabolite PST3093 shows a more favorable therapeutic profile as compared to the parent drug, but it is still unsuitable for chronic usage. Novel PST3093 derivatives have been recently developed for oral (chronic) HF treatment; compound 8 was selected among them and here characterized.

Methods

Effects of compound 8 were evaluated in a context of SERCA2a depression, by using streptozoto

SUBMITTER: Arici M 

PROVIDER: S-EPMC10797746 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature