Constriction to ETB receptor agonists, BQ-3020 and sarafotoxin s6c, in human resistance and capacitance vessels in vivo

Br J Clin Pharmacol. 2000 Jul;50(1):27-30. doi: 10.1046/j.1365-2125.2000.00213.x.

Abstract

Aims: The aim of the study was to examine the effects of the ETB receptor selective agonists sarafotoxin S6c (SFTX6c) and BQ-3020 on the forearm resistance and capacitance vessels in healthy subjects in vivo.

Methods: The local response to intra-arterial or intravenous infusion of SFTX6c (5 pmol min-1) or BQ-3020 (50 pmol min-1) was assessed, on separate occasions, in eight healthy men (aged 20-28 years). Data (mean +/- s.e.mean) were examined by ANOVA. Results are expressed as percentage change from baseline at 90 min.

Results: SFTX6c and BQ-3020 reduced forearm blood flow, following local intra-arterial infusion (-25 +/- 7% and -27 +/- 7%, respectively; P < 0.001) and reduced hand vein diameter, following local intravenous infusion (-30 +/- 8% and -16 +/- 7%, respectively; P < 0.001).

Conclusions: We have shown that locally active infusions of the selective ETB receptor agonists SFTX6c and BQ-3020 cause arterial constriction and venoconstriction in healthy human blood vessels in vivo. These results indicate that ETB receptor stimulation may mediate vasoconstriction in humans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Blood Flow Velocity / drug effects
  • Endothelins / administration & dosage*
  • Forearm / blood supply*
  • Heart Rate / drug effects
  • Humans
  • Infusions, Intra-Arterial
  • Infusions, Intravenous
  • Male
  • Peptide Fragments / administration & dosage*
  • Receptor, Endothelin B
  • Receptors, Endothelin / agonists*
  • Vascular Capacitance / drug effects*
  • Vascular Resistance / drug effects*
  • Vasoconstriction / drug effects*
  • Vasoconstrictor Agents / administration & dosage*
  • Viper Venoms / administration & dosage*

Substances

  • Endothelins
  • Peptide Fragments
  • Receptor, Endothelin B
  • Receptors, Endothelin
  • Vasoconstrictor Agents
  • Viper Venoms
  • sarafotoxins s6
  • BQ 3020