Document Detail

Dilation of epicardial coronary arteries by the G protein-coupled estrogen receptor agonists G-1 and ICI 182,780.
MedLine Citation:
PMID:  20639684     Owner:  NLM     Status:  MEDLINE    
Endogenous estrogens protect from coronary artery disease in premenopausal women, but the mechanisms involved are only partly understood. This study investigated whether activation of the novel G protein-coupled estrogen receptor (GPER, formerly known as GPR30) affects coronary artery tone, and whether this is affected by concomitant blockade of estrogen receptors (ER) alpha and beta. Rings of epicardial porcine coronary arteries suspended in organ chambers were precontracted with prostaglandin F(2)alpha, and direct effects of G-1 (GPER agonist) and ICI 182,780 (GPER agonist and ERalpha/ERbeta antagonist) were determined. In addition, indirect effects on contractility to endothelin-1 and serotonin (a vasoconstrictor released from aggregating platelets during acute myocardial infarction) were assessed. ICI 182,780 and G-1 caused acute dilation of coronary arteries to a comparable degree (p < 0.05 vs. solvent control). Both GPER agonists attenuated contractions to endothelin-1 (p < 0.05 vs. ethanol), but not to serotonin (n.s.). In summary, these findings provide evidence for direct and indirect coronary artery dilator effects of GPER independent of ERalpha and ERbeta, and are the first demonstration of arterial vasodilation in response to ICI 182,780.
Matthias R Meyer; Oliver Baretella; Eric R Prossnitz; Matthias Barton
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2010-07-17
Journal Detail:
Title:  Pharmacology     Volume:  86     ISSN:  1423-0313     ISO Abbreviation:  Pharmacology     Publication Date:  2010  
Date Detail:
Created Date:  2010-08-09     Completed Date:  2010-12-01     Revised Date:  2014-09-12    
Medline Journal Info:
Nlm Unique ID:  0152016     Medline TA:  Pharmacology     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  58-64     Citation Subset:  IM    
Copyright Information:
Copyright 2010 S. Karger AG, Basel.
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MeSH Terms
Coronary Vessels / drug effects*,  physiology
Cyclopentanes / pharmacology*
Endothelin-1 / pharmacology
Estradiol / analogs & derivatives*,  pharmacology
Estrogen Receptor alpha / agonists*,  antagonists & inhibitors,  metabolism
Estrogen Receptor beta / agonists*,  antagonists & inhibitors,  metabolism
Pericardium / drug effects*,  physiology
Quinolines / pharmacology*
Receptors, G-Protein-Coupled / agonists*,  antagonists & inhibitors,  metabolism
Serotonin / pharmacology
Vasodilation / drug effects*
Grant Support
Reg. No./Substance:
0/1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinolin-8-yl)ethanone; 0/Cyclopentanes; 0/Endothelin-1; 0/Estrogen Receptor alpha; 0/Estrogen Receptor beta; 0/Quinolines; 0/Receptors, G-Protein-Coupled; 22X328QOC4/fulvestrant; 333DO1RDJY/Serotonin; 4TI98Z838E/Estradiol

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