Activation of the G protein-coupled estrogen receptor, but not estrogen receptor α or β, rapidly enhances social learning

Ervin, Kelsy S.J.; Mulvale, Erin; Gallagher, Nicola; Roussel, Véronique; Choleris, Elena

doi:10.1016/j.psyneuen.2015.04.002

Cited by 50 publications

(38 citation statements)

References 108 publications

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“…This extends previous reports that PPT decreases food intake within 3–6h in rats (Santollo et al, 2007) and 8h in mice (Ervin et al, 2015). Our findings also demonstrate that lower doses of PPT than used previously (Roesch, 2006; Santollo et al, 2007; Thammacharoen et al, 2009) promote robust decreases in food intake that occur with minimal delay, as female rats typically consume their first nocturnal meal within 1h of dark onset (Eckel et al, 2000).…”

Section: Discussionsupporting

confidence: 91%

“…For example, a 6μg/kg dose of G-1 enhanced social learning in a social transmission of food preference test in female mice at 30min and 2h, but not at 8h (Ervin et al, 2015). In light of these findings, we examined whether similarly low doses of G-1 would be effective in our feeding paradigm.…”

Section: Discussionmentioning

confidence: 99%

“…The higher range of G-1 doses was chosen to be consistent with a previous study investigating the effect of G-1 on food intake in guinea pigs (Washburn et al, 2013). The lower range of G-1 doses was based on preliminary results from our lab and a previous study examining the effects of G-1 on social learning in mice (Ervin et al, 2015). …”

Section: Methodsmentioning

confidence: 99%

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Selective activation of estrogen receptors, ERα and GPER-1, rapidly decreases food intake in female rats

Butler

Hildebrandt

Eckel

2018

Hormones and Behavior

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Many of estradiol’s behavioral effects are mediated, at least partially, via extra-nuclear estradiol signaling. Here, we investigated whether two estrogen receptor (ER) agonists, targeting ERα and G protein-coupled ER-1 (GPER-1), can promote rapid anorexigenic effects. Food intake was measured in ovariectomized (OVX) rats at 1, 2, 4, and 22h following subcutaneous (s.c.) injection of an ERα agonist (PPT; 0–200μg/kg), a GPER-1 agonist (G-1; 0–1600μg/kg), and a GPER-1 antagonist (G-36; 0–80μg/kg). To investigate possible cross-talk between ERα and GPER-1, we examined whether GPER-1 blockade affects the anorexigenic effect of PPT. Feeding was monitored in OVX rats that received s.c. injections of vehicle or 40μg/kg G-36 followed 30min later by s.c. injections of vehicle or 200μg/kg PPT. Selective activation of ERα and GPER-1 alone decreased food intake within 1h of drug treatment, and feeding remained suppressed for 22h following PPT treatment and 4h following G-1 treatment. Acute administration of G-36 alone did not suppress feeding at any time point. Blockade of GPER-1 attenuated PPT’s rapid (within 1h) anorexigenic effect, but did not modulate PPT’s ability to suppress food intake at 2, 4 and 22h. These findings demonstrate that selective activation of ERα produces a rapid (within 1h) decrease in food intake that is best explained by a non-genomic signaling pathway and thus implicates the involvement of extra-nuclear ERα. Our findings also provide evidence that activation of GPER-1 is both sufficient to suppress feeding and necessary for PPT’s rapid anorexigenic effect.

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Section: Discussionsupporting

confidence: 91%

Section: Discussionmentioning

confidence: 99%

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Selective activation of estrogen receptors, ERα and GPER-1, rapidly decreases food intake in female rats

Butler

Hildebrandt

Eckel

2018

Hormones and Behavior

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“…Short term application of a GPER1 agonist also enhances spatial recognition memory in rats; an effect that parallels the actions of E2 (Hawley et al, 2014). Furthermore activation of GPER1, but not ERα or ERβ, mirrors the rapid enhancement of social learning induced by E2 (Ervin et al, 2015). But, emerging evidence indicates that GPER1 enhances hippocampal memory via distinct signalling pathways to E2 (Frick, 2015), suggesting that the effects of GPER1 on memory may be independent of E2.…”

Section: Estrogen and Memory And Cognitionmentioning

confidence: 95%

Emerging roles for the novel estrogen-sensing receptor GPER1 in the CNS

2017

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Keywords: G protein coupled estrogen receptor, hippocampal synaptic function; receptor trafficking; learning and memory; neuroprotection; synaptic plasticity. Estrogens play a key role in regulating reproductive and neuroendocrine function by activating classical nuclear steroid receptors that act as ligand gated transcription factors.However evidence is growing that estrogens also promote rapid non-genomic responses via activation of membrane-associated estrogen receptors. The G protein-coupled estrogen receptor (GPER1; also known as GPR30) has been identified as one of the main estrogensensitive receptors responsible for the rapid non-genomic actions of estrogen. In recent years, our understanding of the CNS actions of GPER1s has significantly increased following the development of selective pharmacological tools and via the use of transgenic technologies to knockout GPER1 in mice. Here we review recent advances that have been made to uncover the role of GPER1s in the CNS.Introduction.

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“…Different from the genomic actions of estrogen, the activation of GPER-1 do not elicit feminizing aspects [23]. It has been demonstrated that G-1 improves the cognitive abilities and social learning of mice [24,25]. It may also possess anxiolytic potential in mice [26,27]; and potential antineoplasic effects, as it is capable of inhibiting the proliferation of cervical, adrenocortical carcinoma and breast tumor cells [28][29][30].…”

Section: Nanocarriers Effects On the Intracellular Delivery Of Fitc Imentioning

confidence: 99%

Development and optimization of G-1 polymeric nanoparticulated and liposomal systems for central nervous system applications

Listik¹

2018

Neurol Disord Therap

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Among many nanotechnological applications, the therapeutical use of nanocarriers is of relevance. G-1, a G-protein estrogen receptor (GPER-1) selective agonist, was encapsulated in polymeric nanoparticles and liposomes modified for central nervous system applications. GPER-1 signals through the rapid estrogen pathway, which is linked with neuroprotection and anti-inflammatory phenomena. Polyssorbate-80-coated PLGA nanoparticles and anti-transferrin antibody labelled immunoliposomes were synthesized. The nanoparticles were obtained by the oil-in-water emulsion method followed by sonication. This synthesis was optimized in terms of surfactant (DMAB or DDAB), sonication regime, T-80 solution dispersion volume and size of stirrer on the size, polidispersity and zeta potential of the nanoparticles. Immunoliposomes containing either DPPC:CH:DSPE-PEG 2000 or DOPC:CH:DSPE-PEG 2000 at 4:1:0.2 molar proportions and DSPE-PEG 2000 -Transferrin(mAb); were obtained by the lipid film hydration method followed by sonication. DMAB tends to produce more monodisperse and stable particles. Moreover, immunoliposomes obtained with DOPC are smaller than those with DPPC. In vitro experiments were performed with Neuro-2a and/or SHSY5Y cells. The results show that T-80-coated NPs do not possess cytotoxicity at low dilutions (324 µg/mL) and are internalized within 24 h. On the other hand, immunoliposomes did not reveal cytotoxicity and were internalized in neurons in less than 30 min. G-1 was encapsulated in both systems, in which PLGA nanoparticles revealed a much lower encapsulation efficiency (41,45 ± 4,05%) than immunoliposomes (97,17 ± 2,84%). These process optimizations may elucidate many aspects of nanocarrier synthesis. It is also believed that G-1-loaded nanocarriers may be efficient for the treatment of several central nervous system diseases more efficiently.

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Activation of the G protein-coupled estrogen receptor, but not estrogen receptor α or β, rapidly enhances social learning

Cited by 50 publications

References 108 publications

Selective activation of estrogen receptors, ERα and GPER-1, rapidly decreases food intake in female rats

Selective activation of estrogen receptors, ERα and GPER-1, rapidly decreases food intake in female rats

Emerging roles for the novel estrogen-sensing receptor GPER1 in the CNS

Development and optimization of G-1 polymeric nanoparticulated and liposomal systems for central nervous system applications

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