1 It has been proposed that the cardiovascular protective actions of 17 bet
a-oestradiol may involve calcium antagonistic actions. We have examined the
effects of 17 beta-oestradiol on contractions to noradrenaline and KCl in
male rat small mesenteric artery and aorta.
2 In rat mesenteric artery, 17 beta-oestradiol (10 mu m) significantly redu
ced the maximum contraction to noradrenaline (67.7 +/- 5.8% of control) and
KCl (38.8 +/- 3.1% of control) without affecting potency.
3 In rat aorta, 17 beta-oestradiol (10 mu m) also significantly reduced con
tractions to noradrenaline (77.5 +/- 4.8% of control), and the effects were
mimicked by droloxifene (10 mu m). The effect of oestrogen was not prevent
ed by the protein synthesis inhibitor cycloheximide (10 mu m). In experimen
ts carried out in calcium-free solution in which calcium stores were deplet
ed, 17 beta-oestradiol (10 mu m) significantly reduced the contraction to c
alcium restoration in rat aorta.
4 In aorta from female rats, 17 beta-oestradiol (10 mu m) significantly red
uced contractions to noradrenaline (73.6 +/- 10.8% of control), but this ef
fect of oestrogen was not prevented by cycloheximide (10 mu m).
5 In summary, 17 beta-oestradiol diminishes the maximum contractile respons
e to noradrenaline in both rat small mesenteric artery and aorta, an effect
which at least in the aorta is mimicked by the oestrogen receptor antagoni
st/partial agonist droloxifene, and may be due to restriction of calcium en
try by a nongenomic action.