Abstract
We have synthesized a library of estrogen analogues, including enantiomers of estradiol and A-ring substituted estrogens. These compounds have reduced or no binding to either estrogen receptor-alpha or estrogen receptor-beta, exhibit enhanced neuroprotective activity in in vitro models, and are potent in protecting brain tissue from cerebral ischemia/reperfusion injury. These potent, nonfeminizing estrogen analogues are prime candidates for use in stroke neuroprotection.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Disease Models, Animal
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Estradiol Congeners / chemistry
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Estradiol Congeners / pharmacology*
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Estradiol Congeners / therapeutic use
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Humans
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Neuroprotective Agents / pharmacology*
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Neuroprotective Agents / therapeutic use
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Rats
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Receptors, Estrogen
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Reperfusion Injury / drug therapy*
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Stroke / drug therapy*
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Structure-Activity Relationship
Substances
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Estradiol Congeners
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Neuroprotective Agents
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Receptors, Estrogen