1. Istaroxime stimulates SERCA2a and accelerates calcium cycling in heart failure by relieving phospholamban inhibition
- Author
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Giuseppe Bianchi, Maria Rosa Moncelli, Isabella Molinari, Cristina Reina, Francesco Tadini-Buoninsegni, Paolo Barassi, Gianluca Bartolommei, Mara Ferrandi, Maria Grazia Tripodi, and Patrizia Ferrari
- Subjects
Pharmacology ,Inotrope ,medicine.medical_specialty ,Lusitropy ,SERCA ,business.industry ,chemistry.chemical_element ,Calcium ,medicine.disease ,Phospholamban ,Contractility ,Istaroxime ,Endocrinology ,chemistry ,Heart failure ,Internal medicine ,medicine ,business - Abstract
Background and Purpose Calcium handling is known to be deranged in heart failure. Interventions aimed at improving cell Ca2+ cycling may represent a promising approach to heart failure therapy. Istaroxime is a new luso-inotropic compound that stimulates cardiac contractility and relaxation in healthy and failing animal models and in patients with acute heart failure (AHF) syndrome. Istaroxime is a Na-K ATPase inhibitor with the unique property of increasing sarcoplasmic reticulum (SR) SERCA2a activity as shown in heart microsomes from humans and guinea pigs. The present study addressed the molecular mechanism by which istaroxime increases SERCA2a activity.
- Published
- 2013