GPER/GPR30 and Regulation of Vascular Tone and Blood Pressure

Author(s): Matthias R. Meyer, Eric R. Prossnitz, Matthias Barton

Journal Name: Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Under Re-organization)
Formerly Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents

Volume 11 , Issue 4 , 2011


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 estrogendependent 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.

Keywords: Blood pressure, endothelium, hormone therapy, hypertension, menopause, nitric oxide, vasodilation

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Article Details

Year: 2011
Page: [255 - 261]
Pages: 7
DOI: 10.2174/1871522211108040255
Price: $65

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