Pivotal role of α2 Na+ pumps and their high affinity ouabain binding site in cardiovascular health and disease

J Physiol. 2016 Nov 1;594(21):6079-6103. doi: 10.1113/JP272419. Epub 2016 Jul 31.

Abstract

Reduced smooth muscle (SM)-specific α2 Na+ pump expression elevates basal blood pressure (BP) and increases BP sensitivity to angiotensin II (Ang II) and dietary NaCl, whilst SM-α2 overexpression lowers basal BP and decreases Ang II/salt sensitivity. Prolonged ouabain infusion induces hypertension in rodents, and ouabain-resistant mutation of the α2 ouabain binding site (α2R/R mice) confers resistance to several forms of hypertension. Pressure overload-induced heart hypertrophy and failure are attenuated in cardio-specific α2 knockout, cardio-specific α2 overexpression and α2R/R mice. We propose a unifying hypothesis that reconciles these apparently disparate findings: brain mechanisms, activated by Ang II and high NaCl, regulate sympathetic drive and a novel neurohumoral pathway mediated by both brain and circulating endogenous ouabain (EO). Circulating EO modulates ouabain-sensitive α2 Na+ pump activity and Ca2+ transporter expression and, via Na+ /Ca2+ exchange, Ca2+ homeostasis. This regulates sensitivity to sympathetic activity, Ca2+ signalling and arterial and cardiac contraction.

Keywords: artery; cardiac hypertrophy; heart failure; hypertension.

Publication types

  • Review

MeSH terms

  • Angiotensins / metabolism
  • Animals
  • Binding Sites
  • Cardiotonic Agents / pharmacology
  • Cardiovascular System / drug effects
  • Cardiovascular System / metabolism*
  • Humans
  • Hypertension / metabolism*
  • Hypertension / physiopathology
  • Ouabain / pharmacology*
  • Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors
  • Sodium-Potassium-Exchanging ATPase / chemistry
  • Sodium-Potassium-Exchanging ATPase / metabolism*
  • Sympathetic Nervous System / metabolism
  • Sympathetic Nervous System / physiology

Substances

  • Angiotensins
  • Cardiotonic Agents
  • Ouabain
  • Sodium-Potassium-Exchanging ATPase