Ovarian steroids and selective estrogen receptor modulators activity on rat brain NMDA and AMPA receptors

Michel Cyr, Othman Ghribi, Caroline Thibault, Marc Morissette, Michelle Landry, Therese Di Paolo

Research output: Contribution to journalArticle

127 Citations (Scopus)

Abstract

Glutamate and glutamate receptors are well known to play a major excitatory role in the brain. Recent findings on ovarian steroids and selective estrogen receptor modulators (SERMs) activity on rat brain AMPA and NMDA receptors are reviewed. Ovarian steroid withdrawal by ovariectomy is without effect on NMDA and AMPA receptors in most brain regions, except in hippocampus, where it decreases NMDA receptor specific binding, compared to intact rat values. Estradiol treatment increases hippocampal NMDA receptor specific binding of ovariectomized rats while it decreases this binding in frontal cortex and striatum. Estradiol treatment has no effect on AMPA receptor specific binding in hippocampus, but decreases binding in frontal cortex, striatum and nucleus accumbens. Progesterone and estradiol+progesterone treatments decrease NMDA, but not AMPA receptors specific binding in frontal cortex compared to ovariectomized rats. No effect was observed in other brain regions. Tamoxifen and raloxifene are SERMs with varying effects on estrogen responses in mammary, bone and uterine tissues. Tamoxifen and raloxifene have estrogenic activity upon modulation of brain NMDA and AMPA receptors. Using specific ligands for binding autoradiography of NMDA receptor subunits and specific probes for subunits measured by in situ hybridization, it was shown that estradiol and SERMs modulate NR1 and NR2B subunits whereas the NR1/2A subunit remains unchanged. In summary, regional agonist estrogenic activity on brain AMPA and NMDA receptors of tamoxifen and raloxifene, like that of estradiol, is observed, whereas progesterone has limited effects or opposes the estradiol effect.

Original languageEnglish (US)
Pages (from-to)153-161
Number of pages9
JournalBrain Research Reviews
Volume37
Issue number1-3
DOIs
StatePublished - Dec 1 2001

Fingerprint

Selective Estrogen Receptor Modulators
AMPA Receptors
N-Methyl-D-Aspartate Receptors
Steroids
Estradiol
Brain
Frontal Lobe
Tamoxifen
Progesterone
Hippocampus
Nucleus Accumbens
Glutamate Receptors
Ovariectomy
N-Methylaspartate
Autoradiography
In Situ Hybridization
Glutamic Acid
Estrogens
Breast
Ligands

Keywords

  • AMPA
  • Estradiol
  • NMPA
  • Raloxifene
  • Tamoxifen

ASJC Scopus subject areas

  • Neuroscience(all)
  • Clinical Neurology

Cite this

Ovarian steroids and selective estrogen receptor modulators activity on rat brain NMDA and AMPA receptors. / Cyr, Michel; Ghribi, Othman; Thibault, Caroline; Morissette, Marc; Landry, Michelle; Di Paolo, Therese.

In: Brain Research Reviews, Vol. 37, No. 1-3, 01.12.2001, p. 153-161.

Research output: Contribution to journalArticle

Cyr, Michel ; Ghribi, Othman ; Thibault, Caroline ; Morissette, Marc ; Landry, Michelle ; Di Paolo, Therese. / Ovarian steroids and selective estrogen receptor modulators activity on rat brain NMDA and AMPA receptors. In: Brain Research Reviews. 2001 ; Vol. 37, No. 1-3. pp. 153-161.
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