Endothelin receptor blockade does not affect blood pressure or angiotensin II levels in CYP1A1-Ren-2 transgenic rats with acutely induced hypertension

Vascul Pharmacol. 2009 May-Jun;50(5-6):194-9. doi: 10.1016/j.vph.2009.01.002.

Abstract

We found previously that selective blockade of endothelin ETA receptors is superior to nonselective ET(A)/ET(B) in attenuating hypertension and survival rate in Ren-2 transgenic rats (TGR). In the present pilot study, we were interested in whether similar effects will be found in TGR with inducible malignant hypertension (iTGR; official strain name Cyp1A1-Ren-2rats), which were derived from the original Ren-2 transgenic rat strain. Studies were performed in three-month old male iTGR. Treatment with either bosentan, a non-selective ET(A)/ET(B), or with atrasentan, a selective ET(A) receptor blocker, was started on day 2 of the experiment. Feeding with indole-3-carbinole (13C; 03% in rat chow), a natural xenobiotic which activates the Cyplal promoter of the mouse Ren-2 gene, began on day 3 and lasted for 4 days until day 6. Systolic BP, body weight, plasma ANG II and tissue ANG II and ET-1 concentrations were determined daily. Severe hypertension developed as early as 1 day after beginning of 13C feeding which was accompanied by a significant reduction in body weight and by increases in plasma and tissue ANG II and left ventricle ET-1 concentrations. Atrasentan or bosentan had no effects on the rise in BP or plasma and tissue ANG II concentrations but prevented the rise in heart ventricle ET-1 concentration. Our data show that blockade of the ET system does not prevent or attenuate the rapid development of severe hypertension in iTGR; a long-term protective effect of ET blockade on cardiac (and renal) damage, however, cannot be excluded and awaits further investigations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin II / blood
  • Angiotensin II / metabolism*
  • Animals
  • Antihypertensive Agents / pharmacology
  • Atrasentan
  • Blood Pressure / drug effects*
  • Bosentan
  • Cytochrome P-450 CYP1A1 / drug effects
  • Cytochrome P-450 CYP1A1 / genetics*
  • Disease Models, Animal
  • Endothelin Receptor Antagonists*
  • Endothelin-1
  • Heart Ventricles / metabolism
  • Hypertension / chemically induced*
  • Hypertension / drug therapy*
  • Indoles / adverse effects
  • Kidney / metabolism
  • Male
  • Pyrrolidines / pharmacology
  • Rats
  • Rats, Transgenic
  • Renin / genetics*
  • Sulfonamides / pharmacology

Substances

  • Antihypertensive Agents
  • Endothelin Receptor Antagonists
  • Endothelin-1
  • Indoles
  • Pyrrolidines
  • Ren2 protein, rat
  • Sulfonamides
  • Angiotensin II
  • indole-3-carbinol
  • Cytochrome P-450 CYP1A1
  • Renin
  • Bosentan
  • Atrasentan