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

Amy Alexander, Andrew J. Irving, Jenni Harvey (Lead / Corresponding author)

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    Abstract

    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 estrogen-sensitive 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.

    Original languageEnglish
    Pages (from-to)652-660
    Number of pages9
    JournalNeuropharmacology
    Volume113
    Issue numberPart B
    Early online date5 Jul 2016
    DOIs
    Publication statusPublished - Feb 2017

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