Acute effects of oestrogen receptor subtype-specific agonists on vascular contractility

Sandra Montgomery, Linda Shaw, Nick Pantelides, Michael Taggart, Clare Austin

Research output: Contribution to journalArticle

32 Citations (Scopus)

Abstract

This study shows for the first time that both the putatively selective oestrogen receptor alpha and oestrogen receptor beta agonists PPT (4,4',4"-(4-propyl-[(1)H]-pyrazole-1,3,5-triyl) tris-phenol) and DPN (2,3-bis(4-hydroxyphenyl)-propionitrile) can acutely relax precontracted isolated rat mesenteric arteries at pharmacological (i.e. micro M) concentrations. When compared to responses observed to similar concentrations of 17beta-oestrogen obtained on the same tissues, PPT had a significantly greater vasodilatory effect, while DPN had a significantly smaller effect. All responses were rapid being complete within 5 min exposure time. Thus, both PPT and DPN can acutely relax isolated mesenteric arteries with the relative potency of PPT>17beta-oestrogen>DPN.

Original languageEnglish
Pages (from-to)1249-53
Number of pages5
JournalBritish Journal of Pharmacology
Volume139
Issue number7
DOIs
Publication statusPublished - 31 Aug 2003

Keywords

  • Animals
  • Dose-Response Relationship, Drug
  • Estradiol/pharmacology
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Female
  • In Vitro Techniques
  • Male
  • Mesenteric Arteries
  • Muscle, Smooth, Vascular/drug effects
  • Nitriles/pharmacology
  • Phenols/pharmacology
  • Pyrazoles/pharmacology
  • Rats
  • Rats, Wistar
  • Receptors, Estrogen/agonists
  • Selective Estrogen Receptor Modulators/pharmacology
  • Time Factors
  • Vasoconstriction/drug effects

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