Distinct effects of bosentan on NO-dependent vasodilation and calcium influx in heterozygous Ren-2 transgenic rats on high-salt diet

Physiol Res. 2019 Oct 25;68(5):717-725. doi: 10.33549/physiolres.934192. Epub 2019 Aug 19.

Abstract

Our studies in hypertensive Ren-2 transgenic rats (TGR) demonstrated that chronic administration of atrasentan (ETA receptor antagonist) decreased blood pressure by reduced Ca2+ influx through L-type voltage-dependent calcium channels (L-VDCC) and attenuated angiotensin II-dependent vasoconstriction. We were interested whether bosentan (nonselective ET(A)/ET(B) receptor antagonist) would have similar effects. Young 4-week-old (preventive study) and adult 8-week-old (therapeutic study) heterozygous TGR and their normotensive Hannover Sprague-Dawley (HanSD) controls were fed normal-salt (NS, 0.6 % NaCl) or high-salt (HS, 2 % NaCl) diet for 8 weeks. An additional group of TGR fed HS was treated with bosentan (100 mg/kg/day). Bosentan had no effect on BP of TGR fed high-salt diet in both the preventive and therapeutic studies. There was no difference in the contribution of angiotensin II-dependent and sympathetic vasoconstriction in bosentan-treated TGR compared to untreated TGR under the condition of high-salt intake. However, bosentan significantly reduced NO-dependent vasodilation and nifedipine-sensitive BP component in TGR on HS diet. A highly important correlation of nifedipine-induced BP change and the BP after L-NAME administration was demonstrated. Although bosentan did not result in any blood pressure lowering effects, it substantially influenced NO-dependent vasodilation and calcium influx through L-VDCC in the heterozygous TGR fed HS diet. A significant correlation of nifedipine-induced BP change and the BP after L-NAME administration suggests an important role of nitric oxide in the closure of L-type voltage dependent calcium channels.

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Bosentan / pharmacology*
  • Calcium Channels, L-Type / metabolism*
  • Calcium Signaling / drug effects*
  • Disease Models, Animal
  • Endothelin Receptor Antagonists / pharmacology*
  • Heterozygote
  • Hypertension / drug therapy*
  • Hypertension / genetics
  • Hypertension / metabolism
  • Hypertension / physiopathology
  • Male
  • Nitric Oxide / metabolism*
  • Rats, Sprague-Dawley
  • Rats, Transgenic
  • Renin / genetics*
  • Sodium Chloride, Dietary*
  • Vasodilation / drug effects*

Substances

  • Calcium Channels, L-Type
  • Endothelin Receptor Antagonists
  • Sodium Chloride, Dietary
  • mRen2 protein, rat
  • Nitric Oxide
  • Renin
  • Bosentan