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Acute effects of oestrogen receptor subtype‐specific agonists on vascular contractility
Author(s) -
Montgomery Sandra,
Shaw Linda,
Pantelides Nick,
Taggart Michael,
Austin Clare
Publication year - 2003
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0705368
Subject(s) - oestrogen receptor , medicine , endocrinology , mesenteric arteries , contractility , vasodilation , agonist , receptor , chemistry , potency , vasoconstriction , artery , in vitro , biochemistry , cancer , breast cancer
This study shows for the first time that both the putatively selective oestrogen receptor α and oestrogen receptor β 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. μ M ) concentrations. When compared to responses observed to similar concentrations of 17 β ‐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>17 β ‐oestrogen>DPN. British Journal of Pharmacology (2003) 139 , 1249–1253. doi: 10.1038/sj.bjp.0705368