Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Comparative Study
. 2003 Aug;139(7):1249-53.
doi: 10.1038/sj.bjp.0705368.

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

Affiliations
Comparative Study

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

Sandra Montgomery et al. Br J Pharmacol. 2003 Aug.

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.

PubMed Disclaimer

Figures

Figure 1
Figure 1
A comparison of the effects of 17β-oestradiol and (a) PPT and (b) DPN on the contractility of isolated rat mesenteric arteries precontracted with KPSS alone. **P<0.005.

References

    1. AUSTIN C.E. Chronic and acute effects of oestrogens on vascular contractility. J. Hypertens. 2000;18:1365–1378. - PubMed
    1. CREWS J.K., KHALIL R.A. Antagonistic effects of 17β-estradiol, progesterone, and testosterone on Ca2+ entry mechanisms of coronary vasoconstriction. Arterioscler. Thromb. Vasc. Biol. 1999;19:1034–1040. - PubMed
    1. GREEN S., WALTER P., KUMAR V., KRUST A., BONERT J.M, ARGOS P., CHAMBON P. Human oestrogen receptor cDNA: sequence, expression and homology to v-erb-A. Nature. 1986;320:134–139. - PubMed
    1. KRAICHELY D.M., SUN J., KATZENELLENBOGEN J.A., KATZENELLENBOGEN B.S. Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-α and estrogen receptor-β. Endocrinology. 2000;141:3534–3545. - PubMed
    1. KUIPER G.G.J.M., ENMARK E., PELTO-HUIKKO M., NILSSON S., GUSTAFSSON J.A. Cloning of a novel estrogen receptor expressed in rat prostrate and ovary. Proc. Natl. Acad. Sci. U.S.A. 1996;93:5925–5930. - PMC - PubMed

Publication types

MeSH terms

LinkOut - more resources