Interactions of exendin-(9-39) with the effects of glucagon-like peptide-1-(7-36) amide and of exendin-4 on arterial blood pressure and heart rate in rats

Regul Pept. 1996 Nov 14;67(1):63-8. doi: 10.1016/s0167-0115(96)00113-9.

Abstract

This study was designed to determine the interactions of peptide exendin-(9-39) with the effect of glucagon-like peptide-1-(7-36) (GLP-1 (7-36)) amide and of exendin-4 on arterial blood pressure and heart rate in the rat. Both GLP-1 (7-36) amide and exendin-4 produced a dose-dependent increase in systolic, diastolic and mean arterial blood pressure, as well as in heart rate, although the effect of exendin-4 was more prolonged. These data indicate a longer functional half-life in vivo for exendin-4 as compared to GLP-1 (7-36) amide, which may have therapeutical applications. The antagonist effect of exendin-(9-39) on these cardiovascular parameters was also tested with 3000 ng of exendin-(9-39) intravenously administered 5 min before i.v. injection of 10 ng of either GLP-1 (7-36) amide or exendin-4. Under these experimental conditions the effect of the latter two peptides on arterial blood pressure and heart rate was blocked. By contrast, single administration of exendin-(9-39) did not modify cardiovascular parameters. These findings indicate that exendin-4 is an agonist and that exendin-(9-39) is an antagonist of the action of GLP-1 (7-36) amide on arterial blood pressure and heart rate. Therefore, the action of GLP-1 (7-36) amide on these parameters seems to be mediated through its own receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Pressure / drug effects*
  • Exenatide
  • Glucagon
  • Glucagon-Like Peptide 1
  • Glucagon-Like Peptides
  • Heart Rate / drug effects*
  • Male
  • Peptide Fragments / agonists
  • Peptide Fragments / antagonists & inhibitors
  • Peptide Fragments / pharmacology*
  • Peptides / metabolism
  • Peptides / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Venoms / chemistry

Substances

  • Peptide Fragments
  • Peptides
  • Venoms
  • glucagon-like peptide 1 (7-36)amide
  • exendin (9-39)
  • Glucagon-Like Peptides
  • Glucagon-Like Peptide 1
  • Glucagon
  • Exenatide