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 language | English |
|---|---|
| Pages (from-to) | 1249-53 |
| Number of pages | 5 |
| Journal | British Journal of Pharmacology |
| Volume | 139 |
| Issue number | 7 |
| DOIs | |
| Publication status | Published - 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