title: GPER/GPR30 and Regulation of Vascular Tone and Blood Pressure.
abstract: Natural estrogens such as 17β-estradiol are endogenous vasodilators and have been implicated in the gender differences of hypertension. These hormones activate estrogen receptors ERα and ERβ, which mediate part of estrogen-dependent vasodilation. In addition, a novel G protein-coupled estrogen-binding receptor termed GPER/GPR30 has been identified that is expressed in the cardiovascular system. Using knock-out animals or drugs selectively targeting GPER/GPR30, a significant role for this receptor as a mediator of acute estrogen-dependent vasodilation involving nitric oxide (NO) and blood pressure-lowering activity has been demonstrated. The accumulating evidence that GPER/GPR30 is responsible for control of vascular tone indicates that this receptor may represent a novel drug target for pharmacologic treatment of hypertension in postmenopausal women and possibly also men.
authors.affiliation: Molecular Internal Medicine, University of Zurich, Zurich, Switzerland ; Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM, United States.
authors.forename: Matthias R
authors.initials: MR
authors.lastname: Meyer
authors.affiliation: Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM, United States.
authors.forename: Eric R
authors.initials: ER
authors.lastname: Prossnitz
authors.affiliation: Molecular Internal Medicine, University of Zurich, Zurich, Switzerland.
authors.forename: Matthias
authors.initials: M
authors.lastname: Barton
keywords: Blood Pressure; Endothelium; Hormone Therapy; Hypertension; Menopause; Nitric Oxide; Vasodilation