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

被引:31
作者
Montgomery, S
Shaw, L
Pantelides, N
Taggart, M
Austin, C
机构
[1] Manchester Royal Infirm, Dept Med, Smooth Muscle Physiol Grp, Manchester M13 9WL, Lancs, England
[2] Univ Manchester, Maternal & Fetal Hlth Res Ctr, Manchester M13 9WL, Lancs, England
关键词
oestrogen receptor agonists; artery; contractility;
D O I
10.1038/sj.bjp.0705368
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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-[H-1]-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. muM) 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.
引用
收藏
页码:1249 / 1253
页数:5
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