Selective estrogen receptor modulators: tissue actions and potential for CNS protection.

  title={Selective estrogen receptor modulators: tissue actions and potential for CNS protection.},
  author={Marguerite T. Littleton-Kearney and Nancy L. Ostrowski and David A. Cox and Mark I. Rossberg and Patricia D. Hurn},
  journal={CNS drug reviews},
  volume={8 3},
Significant physiologic changes occur during menopause. Evidence exists to suggest that estrogen may be neuroprotective under specific conditions. However, there are limitations in the neuroprotection afforded by standard hormone therapy. Accordingly, alternative agents with selected estrogenic effects may hold even greater promise rather than conventional hormone replacement therapy for the prevention and treatment of CNS injury. Recently, a variety of selective estrogen receptor modulators… 

Estrogen and selective estrogen receptor modulators

Research is still needed to optimize combined or estrogen alone hormone replacement therapy options as well as the prevention/management of cerebrovascular/central nervous system disorders and neuroprotective role for SERMs in normal and injured brain.

Astrocytes Mediate Protective Actions of Estrogenic Compounds after Traumatic Brain Injury

It is concluded that the use of estrogenic compounds to modulate astrocytic properties is a promising therapeutic approach for the treatment of TBI.

Molecular and Clinical Evidence for the Unique Nature of Individual Selective Estrogen Receptor Modulators

This paper first examines the biochemical nature of selective estrogen receptor modulators (SERMs), which include the estrogens, and the known mechanisms by which they can exhibit tissue-selective agonist/antagonist activities.

Neuroprotective effects of estrogens and androgens in CNS inflammation and neurodegeneration

Effects of estrogen receptor modulators on cytoskeletal proteins in the central nervous system

Raloxifene, tamoxifen, and tibolone modulate some cytoskeletal proteins such as tau, microtuble-associated protein 1 (MAP1), MAP2, neurofilament 38 (NF38) by different mechanisms of action and at different levels: neuronal microfilaments, intermediate filaments, and microtubule-associated proteins.

Role of Estrogen Treatment in the Management of Schizophrenia

An overview of different applications of adjunctive estrogen as a possible treatment for symptoms of schizophrenia in both men and women is provided.

Estrogen-Mediated Neuroprotection: Hope to Combat Neuronal Degeneration and Synaptic Plasticity Post-menopause

The findings have revealed that ovariectomy or natural aging leads to decreased synaptic activity, degenerative cytoarchitectural changes and altered protein levels in hippocampal neurons, and it was seen that long-term estrogen therapy maintains the synaptic plasticity, regulates apoptotic proteins and affords neuroprotection to the hippocampusal neurons through both the nuclear and membrane estrogen receptor mediated pCREB and MAPK activation.

Raloxifene as Treatment for Various Types of Brain Injuries and Neurodegenerative Diseases: A Good Start †

  • L. Veenman
  • Biology
    International journal of molecular sciences
  • 2020
An overview of potential treatments of neurodegenerative disease by raloxifene is presented, and attention is paid to subcellular molecular biological pathways that may be involved.

Complexities of oestrogen in stroke.

The issue of the neuroprotective effects of oestrogen in stroke is addressed in the present review, along with potential mechanisms of action, and the translational capacity of pre-clinical research.



Neuroprotective effects of estrogens: potential mechanisms of action

  • P. GreenJ. Simpkins
  • Biology, Psychology
    International Journal of Developmental Neuroscience
  • 2000

Therapeutic potential of selective estrogen receptor modulators.

Minireview: Neuroprotective Effects of Estrogen-New Insights into Mechanisms of Action.

Estradiol appears to act at two levels: 1) it decreases the risk of disease or injury; and/or 2) it increases the extent of injury incurred by suppressing the neurotoxic stimulus itself or increasing the resilience of the brain to a given injury.

Estrogen as a Neuroprotectant in Stroke

  • P. HurnI. Macrae
  • Medicine, Psychology
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • 2000
Gender-specific aspects of clinical and experimental stroke and results of estrogen treatment on outcome in animal models of cerebral ischemia are summarized, and potential vascular and parenchymal mechanisms by which estrogen salvages brain are discussed.

What Would Be the Properties of an Ideal SERM?

The latest and largest randomized clinical trials have demonstrated a beneficial role in short‐term memory in nondemented women, in contrast to the absence of such benefit in improving symptoms in women with Alzheimer's disease.

Selective Estrogen Receptor Modulators: An Alternative to Hormone Replacement Therapy

  • H. BryantW. Dere
  • Biology
    Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine
  • 1998
It is clear that for raloxifene, both the estrogen agonist effects on bone and cholesterol metabolism as well as the estrogen antagonist effects in uterine and mammary tissue involve high affinity interaction with the estrogen receptor.

Selective Estrogen Receptor Modulator Effects in the Rat Brain

While SERMs are not full estrogen receptor agonists in the brain, the agonist/antagonist profiles for individual SERMs may differ among brain areas, raising the possibility of developing new SERMs for selective functions in specific brain areas.

Cellular and molecular mechanisms of estrogen regulation of memory function and neuroprotection against Alzheimer's disease: recent insights and remaining challenges.

  • R. Brinton
  • Biology, Psychology
    Learning & memory
  • 2001
This review focuses on recent advances in knowledge of estrogen action in the brain and those studies that impact the understanding of estrogen regulation of memory function and prevention of degenerative diseases associated with memory systems, such as Alzheimer's disease.