For research use only. Not Intended for Therapeutic Use!
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Ouabain Octahydrate inhibits Na(+)/K(+) ATPase, regulates transcription of MDR and MRP.
Ouabain Octahydrate is a Na(+)/K(+) ATPase inhibitor. Ouabain (100 nM) inhibits ATPase activities with 25% . Ouabain (0.1 μM-1.0 μM) inhibits the Na+ pump and increases stored Ca2+ in cultured rat astrocytes. High Ouabain affinity isoforms (alpha2 in astrocytes, alpha3 in neurons and myocytes) are confined to a reticular distribution within the PM that paralleled underlying endoplasmic or sarcoplasmic reticulum . Ouabain (0.5-1.0 mM) increases the levels of alpha1 and beta1 mRNAs, whereas it decreases those of alpha2 and beta2 mRNAs in cultured rat astrocytes. Ouabain increases alpha1 and beta1, but not alpha2 and beta2, proteins, and that the isoforms in control and ouabain-treated cultures. The ouabain-induced increase in alpha1 mRNA is blocked by cycloheximide (10 mM), the intracellular Ca2+ chelator 1,2-bis(2-aminophenoxy)ethane-N,N,N/',N/'-tetraacetic acid tetraacetoxymethyl ester (30 mM), and FK506 (1 nM) in cultured rat astrocytes .
Ouabain (14.4 mg/kg.d s.c. intermittent) further increases total peripheral resistance (TPR) in rats with heart failure due to myocardial infarction (MI), while continuous Ouabain treatment normalized TPR in rats. Ouabain (14.4 mg/kg.d s.c. continuous) significantly improves basal and maximal CO (basal: 83 mL/min; maximal: 134 mL/min) .
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