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(Stroke. 2004;35:2648.)
© 2004 American Heart Association, Inc.

Articles

Estrogen-Like Compounds for Ischemic Neuroprotection

James W. Simpkins, PhD; Shao-Hua Yang, MD PhD; Ran Liu, MD; Evelyn Perez, PhD; Zu Yun Cai, PhD; Douglas F. Covey, PhD Pattie S. Green, PhD

From the Department of Pharmacology & Neuroscience (J.W.S., S.-H.Y., R.L., E.P.), University of North Texas Health Science Center, Fort Worth, Texas; the Department of Molecular Biology and Pharmacology (Z.Y.C., D.F.C.), Washington University School of Medicine, St. Louis, Mo; and the Department of Gerontology and Geriatric Medicine (P.S.G.), School of Medicine, University of Washington, Seattle, Wash.

Correspondence to Dr James W. Simpkins, Department of Pharmacology & Neuroscience, 3500 Camp Bowie Blvd, University of North Texas Health Science Center, Fort Worth, TX 76107. E-mail jsimpkin{at}hsc.unt.edu

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- or estrogen receptor-ß, 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.

Key Words: estrogens • estrogen receptors • neuroprotection • stroke

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