Acute effects of oestrogen receptor subtype-specific agonists on vascular contractility.
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.
Montgomery
Sandra
S
Smooth Muscle Physiology Group, Cardiovascular Research, Department of Medicine, Manchester Royal Infirmary, Oxford Road, Manchester M13 9WL.
Shaw
Linda
L
Pantelides
Nick
N
Taggart
Michael
M
Austin
Clare
C
D000818:Animals; D004305:Dose-Response Relationship, Drug; D004958:Estradiol / Q000494:pharmacology; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D008638:Mesenteric Arteries; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology; D009570:Nitriles / Q000494:pharmacology; D010636:Phenols / Q000494:pharmacology; D011720:Pyrazoles / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D011960:Receptors, Estrogen / Q000819:agonists* / Q000502:physiology; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology*; D013997:Time Factors; D014661:Vasoconstriction / Q000187:drug effects; D011422:Propionates
D004958:Estradiol; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D009570:Nitriles; D010636:Phenols; D011720:Pyrazoles; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; C486182:2,3-bis(4-hydroxyphenyl)-propionitrile; D011422:Propionates; C486184:4,4',4''-(4-propyl-((1)H)-pyrazole-1,3,5-triyl) tris-phenol