Literature DB >> 23362079

G protein-coupled estrogen receptor agonist improves cerebral microvascular function after hypoxia/reoxygenation injury in male and female rats.

Takahiro Murata1, Hans H Dietrich, Chuanxi Xiang, Ralph G Dacey.   

Abstract

BACKGROUND AND
PURPOSE: Reduced risk and severity of stroke in adult females are thought to depend on normal levels of endogenous estrogen, which is a known neuro- and vasoprotective agent in experimental cerebral ischemia. Recently, a novel G protein-coupled estrogen receptor (GPER, formerly GPR30) has been identified and may mediate the vasomotor and -protective effects of estrogen. However, the signaling mechanisms associated with GPER in the cerebral microcirculation remain unclear. We investigated the mechanism of GPER-mediated vasoreactivity and also its vasoprotective effect after hypoxia/reoxygenation (H/RO) injury.
METHODS: Rat cerebral penetrating arterioles from both sexes were isolated, cannulated, and pressurized. Vessel diameters were recorded by computer-aided videomicroscopy. To investigate vasomotor mechanism of the GPER agonist (G-1), several inhibitors with or without endothelial impairment were tested. Ischemia/reperfusion injury was simulated using H/RO. Vasomotor responses to adenosine triphophate after H/RO were measured with or without G-1 and compared with controls.
RESULTS: G-1 produced a vasodilatory response, which was partially dependent on endothelium-derived nitric oxide (NO) but not arachidonic acid cascades and endothelial hyperpolarization factor. Attenuation of G-1-vasodilation by the NO synthase inhibitor and endothelium-impairment were greater in vessels from female than male animals. G-1 treatment after H/RO injury fully restored arteriolar dilation to adenosine triphophate compared with controls.
CONCLUSIONS: GPER agonist elicited dilation, which was partially caused by endothelial NO pathway and induced by direct relaxation of smooth muscle cells. Further, GPER agonist restored vessel function of arterioles after H/RO injury and may play an important role in the ability of estrogen to protect the cerebrovasculature against ischemia/reperfusion injury.

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Year:  2013        PMID: 23362079      PMCID: PMC3923380          DOI: 10.1161/STROKEAHA.112.678177

Source DB:  PubMed          Journal:  Stroke        ISSN: 0039-2499            Impact factor:   7.914


  33 in total

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2.  Postischemic estrogen reduces hypoperfusion and secondary ischemia after experimental stroke.

Authors:  L D McCullough; N J Alkayed; R J Traystman; M J Williams; P D Hurn
Journal:  Stroke       Date:  2001-03       Impact factor: 7.914

Review 3.  Estrogen as a neuroprotectant in stroke.

Authors:  P D Hurn; I M Macrae
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5.  Activation of G protein-coupled estrogen receptor induces endothelium-independent relaxation of coronary artery smooth muscle.

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6.  Estrogen modulation of endothelium-derived relaxing factors by human endothelial cells.

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9.  A study of rat intracerebral arterioles: methods, morphology, and reactivity.

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10.  Differential role of PTK and ERK MAPK in superoxide impairment of K(ATP) and K(Ca) channel cerebrovasodilation.

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  28 in total

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Authors:  Eric R Prossnitz; Helen J Hathaway
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Review 2.  GPER modulators: Opportunity Nox on the heels of a class Akt.

Authors:  Eric R Prossnitz
Journal:  J Steroid Biochem Mol Biol       Date:  2017-03-08       Impact factor: 4.292

Review 3.  Recent Advances on the Role of G Protein-Coupled Receptors in Hypoxia-Mediated Signaling.

Authors:  Rosamaria Lappano; Damiano Rigiracciolo; Paola De Marco; Silvia Avino; Anna Rita Cappello; Camillo Rosano; Marcello Maggiolini; Ernestina Marianna De Francesco
Journal:  AAPS J       Date:  2016-02-10       Impact factor: 4.009

Review 4.  International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators.

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Journal:  Pharmacol Rev       Date:  2015-07       Impact factor: 25.468

5.  G protein-coupled estrogen receptor-mediated effects on cytosolic calcium and nanomechanics in brain microvascular endothelial cells.

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Review 6.  Emerging roles of GPER in diabetes and atherosclerosis.

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Review 7.  Alike but not the same: anatomic heterogeneity of estrogen receptor-mediated vasodilation.

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8.  Adaptive increases in expression and vasodilator activity of estrogen receptor subtypes in a blood vessel-specific pattern during pregnancy.

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Review 9.  Estrogen receptor agonists for attenuation of neuroinflammation and neurodegeneration.

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Review 10.  Estrogen biology: new insights into GPER function and clinical opportunities.

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Journal:  Mol Cell Endocrinol       Date:  2014-02-12       Impact factor: 4.102

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