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. Author manuscript; available in PMC: 2015 Oct 1.
Published in final edited form as: Brain Res Bull. 2014 Sep 20;109:22–31. doi: 10.1016/j.brainresbull.2014.09.004

Table 1. Estrogen and SERM derivatives examined for potential neuroprotective functions.

Estrogen and SERM derivatives Estrogen or SERM Functions References
Estrogen derivatives 17β-Estradiol Antioxidant, neuroprotective Chakrabarti et al., 2014; Mosquera et al., 2014
17α-Estradiol Inhibits GABA receptor-induced cell loss McClean and Nuñez, 2008; Rakkestad et al., 2014
Estriol Reduces the disease symptoms in multiple sclerosis (MS) Sicotte et al., 2002; Ziehn et al., 2012
Equilin Used in hormone replacement therapy Sawicki et al., 1999; Okamoto et al., 2010
Triphenylethylene derivatives Tamoxifen Neuroprotection to Aβ-induced toxicity O'Neill et al. 2004; Herrera et al., 2011
4-Hydroxy tamoxifen Neuroprotection to Aβ-induced toxicity O'Neill et al., 2004; Arevalo et al., 2011
Droloxifene Inhibits estrogen mediated neuroprotection Christian, 2001; Zhao et al., 2005
Ospemifene Induces production and release of pro-inflammatory molecules by glial cells Cerciat et al., 2010; Arevalo et al., 2011
Phytoestrogens Coumestrol Protects hippocampal neurons in cerebral ischemia Castro et al., 2012; Castro et al., 2014
Daidzein Decreases cell death and improves synaptic function in oxygen–glucose deprivation (OGD) Schreihofer and Redmond, 2009; Hurtado et al., 2012
Equol Vasorelaxant, anti-oxidant, and neuroprotective in transient focal cerebral ischemia Jackman et al., 2007; Ma et al., 2010.
Formononetin Protects neurons from NMDA-induced excitotoxic injury and neurodegenerative disorders in central nervous system Occhiuto et al., 2008; Occhiuto et al., 2009; Tian et al., 2013
Genistein Reduces oxidative stress, hippocampal neuron death, and cognitive defects in neurodegenerative disorders Azcoitia et al., 2006; Malinowska et al., 2010; Wang et al., 2013
Benzothiophene derivatives Arzoxifene GPR30-dependent and ER-independent neuroprotection Littleton-Kearney et al., 2002; Abdelhamid et al., 2011
Bazedoxifene Anti-inflammatory effects in astrocytes, inhibition of IL-6, IFN-ɣ, and NF-κB p65 transactivation Cerciat et al., 2010; Arevalo et al., 2011
Raloxifene Poor bioavailability, ERα dependent but ERβ and GPR30 independent hypoxia induced neuroprotection Kushwaha et al., 2013; Rzemieniec et al., 2014