Effect of endothelin and BQ123 on ocular blood flow parameters in healthy subjects

Invest Ophthalmol Vis Sci. 2001 Nov;42(12):2949-56.

Abstract

Purpose: To characterize the role of the endothelin system in the blood flow control of the optic nerve head and of the choroid in humans.

Methods: Two studies were performed in healthy subjects. Study 1 was a randomized, placebo-controlled, double-masked, balanced, two-way crossover design and study 2 a three way-way crossover design. In study 1 twelve healthy male subjects received endothelin (ET)-1 in stepwise increasing doses of 1.25, 2.5, and 5 ng/kg x min (each infusion step occurred over 20 minutes) coinfused with BQ123 (60 microg/kg x min) or placebo on two different study days. In study 2 twelve healthy male subjects received two doses of BQ123 (60 or 120 microg/kg x min over 60 minutes) or placebo on three different study days. Measurements of optic nerve head blood flow (ONHBF) and choroidal blood flow (ChBF) were performed with laser Doppler flowmetry in both studies. In study 2 mean flow velocity (MFV) of the ophthalmic artery was assessed with Doppler sonography.

Results: In study 1, ET-1 significantly decreased ONHBF (-22.8% +/- 4.3% at 5 ng/kg x min, P = 0.003 versus baseline) and ChBF (-21.7% +/- 3.2% at 5 ng/kg x min, P = 0.0001 versus baseline). The effect of the highest administered dose of exogenous ET-1 on ONHBF was significantly attenuated (P = 0.04, ANOVA) by coinfusion of BQ123. Effects of exogenous ET-1 on blood flow (2.5 ng/kg x min ET-1 or higher) also were attenuated in the choroid by coinfusion of BQ123 (ChBF: P = 0.03, ANOVA). In study 2, both dosages of BQ123 significantly increased MFV in the ophthalmic artery (60 microg/kg x min, 12.5% +/- 7.3%; 120 microg/kg x min, 17.2% +/- 9.2%, versus baseline; P = 0.001), but did not change blood flow in the ONH or the choroid.

Conclusions: BQ123 antagonizes the effects of exogenously administered ET-1 on blood flow in the ONH and the choroid. The data indicate, however, that ET-1 does not substantially contribute to the regulation of basal vascular tone in these tissues.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antihypertensive Agents / pharmacology*
  • Blood Flow Velocity / drug effects
  • Choroid / blood supply*
  • Cross-Over Studies
  • Double-Blind Method
  • Drug Combinations
  • Endothelin Receptor Antagonists*
  • Endothelin-1 / administration & dosage
  • Endothelin-1 / pharmacology*
  • Humans
  • Infusions, Intravenous
  • Laser-Doppler Flowmetry
  • Male
  • Ophthalmic Artery / diagnostic imaging
  • Ophthalmic Artery / physiology*
  • Optic Disk / blood supply*
  • Peptides, Cyclic / administration & dosage
  • Peptides, Cyclic / pharmacology*
  • Regional Blood Flow
  • Ultrasonography

Substances

  • Antihypertensive Agents
  • Drug Combinations
  • Endothelin Receptor Antagonists
  • Endothelin-1
  • Peptides, Cyclic
  • cyclo(Trp-Asp-Pro-Val-Leu)