Angiotensin II Receptor-Neprilysin Inhibitor Sacubitril/Valsartan Improves Endothelial Dysfunction in Spontaneously Hypertensive Rats

J Am Heart Assoc. 2017 Oct 17;6(10):e006617. doi: 10.1161/JAHA.117.006617.

Abstract

Background: We have previously demonstrated that antihypertensive treatment with renin-angiotensin system inhibitors restores the impaired endothelium-dependent hyperpolarization (EDH)-mediated responses in spontaneously hypertensive rats (SHRs). Herein, we investigated whether the angiotensin II receptor-neprilysin inhibitor sacubitril/valsartan (LCZ696) would improve reduced EDH-mediated responses and whether LCZ696 would exert additional effects on endothelium-dependent and endothelium-independent vasorelaxation compared with an angiotensin II type 1 receptor blocker alone during hypertension.

Methods and results: SHRs were treated for 3 months with either LCZ696 or valsartan, from the age of 8 to 11 months. Age-matched, untreated SHRs and Wistar-Kyoto rats served as controls. Membrane potentials and contractile responses were recorded from the isolated superior mesenteric arteries. Acetylcholine-induced, EDH-mediated responses were impaired in untreated SHRs compared with Wistar-Kyoto rats. EDH-mediated responses were similarly improved in the LCZ696- and valsartan-treated SHRs. No difference was observed in acetylcholine-induced, nitric oxide-mediated relaxations among the 4 groups. Endothelium-independent relaxations in response to a nitric oxide donor, sodium nitroprusside, and those to levcromakalim, an ATP-sensitive K+-channel opener, were similar among the 4 groups; however, the sensitivities to levcromakalim were significantly higher in both LCZ696- and valsartan-treated SHRs.

Conclusions: LCZ696 appears to be as effective as valsartan in improving the impaired EDH-mediated responses during hypertension. LCZ696 and valsartan exert similar beneficial effects on endothelium-independent relaxation via enhanced sensitivity of the ATP-sensitive K+ channel. However, the dual blockade of renin-angiotensin system and neutral endopeptidase with LCZ696 does not appear to provide additional benefit over valsartan alone on vasomotor function in mesenteric arteries of SHRs.

Keywords: endothelial function; endothelial‐derived relaxant factor; hypertension; renin angiotensin system.

Publication types

  • Comparative Study

MeSH terms

  • Aminobutyrates / pharmacology*
  • Angiotensin II Type 1 Receptor Blockers / pharmacology*
  • Animals
  • Antihypertensive Agents / pharmacology*
  • Biphenyl Compounds
  • Blood Pressure / drug effects*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Combinations
  • Endothelium, Vascular / drug effects*
  • Endothelium, Vascular / enzymology
  • Endothelium, Vascular / physiopathology
  • Hypertension / drug therapy*
  • Hypertension / enzymology
  • Hypertension / genetics
  • Hypertension / physiopathology
  • KATP Channels / agonists
  • KATP Channels / metabolism
  • Male
  • Membrane Potentials / drug effects
  • Mesenteric Artery, Superior / drug effects*
  • Mesenteric Artery, Superior / enzymology
  • Mesenteric Artery, Superior / physiopathology
  • Neprilysin / antagonists & inhibitors*
  • Neprilysin / metabolism
  • Protease Inhibitors / pharmacology*
  • Rats, Inbred SHR
  • Renin-Angiotensin System / drug effects
  • Signal Transduction / drug effects
  • Tetrazoles / pharmacology*
  • Time Factors
  • Valsartan
  • Vasodilation / drug effects*
  • Vasodilator Agents / pharmacology*

Substances

  • Aminobutyrates
  • Angiotensin II Type 1 Receptor Blockers
  • Antihypertensive Agents
  • Biphenyl Compounds
  • Drug Combinations
  • KATP Channels
  • Protease Inhibitors
  • Tetrazoles
  • Vasodilator Agents
  • Valsartan
  • Neprilysin
  • sacubitril and valsartan sodium hydrate drug combination