17β-Estradiol induces vasorelaxation in a G-protein-coupled receptor 30-independent manner.
17β-Estradiol (E2) exerts rapid non-genomic vascular effects through activation of its plasma membrane receptors. We tested the hypothesis that E2 induces vasorelaxation through activation of the G-protein-coupled receptor 30 (GPR30) in rat aorta. Rat aortic rings were mounted in organ baths and subjected to contraction followed by relaxation. Whether endothelium was intact or denuded, both E2 and G1, a GPR30 agonist, induced vasorelaxation in concentration-dependent manners. Although G15, a specific GPR30 antagonist, blocked G1-induced vasorelaxation, it did not block E2-induced vasorelaxation. In conclusion, 17β-estradiol induces vasorelaxation in a GPR30-independent manner in rat aorta.
Cardiovascular Research Institute, Kyungpook National University School of Medicine, Daegu, 700-422, Republic of Korea.
Young Mi
YM
Seok
Eun Jin
EJ
Jang
Oliver
O
Reiser
Markus
M
Hager
In Kyeom
IK
Kim
D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004730:Endothelium, Vascular / Q000187:drug effects / Q000378:metabolism; D004958:Estradiol / Q000008:administration & dosage / Q000494:pharmacology*; D004967:Estrogens / Q000008:administration & dosage / Q000494:pharmacology; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects / Q000378:metabolism*; D014664:Vasodilation / Q000187:drug effects*
D004967:Estrogens; C520305:Gper1 protein, rat; D043562:Receptors, G-Protein-Coupled; D004958:Estradiol