Estrogen-like compounds for ischemic neuroprotection.
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.
Simpkins
James W
JW
Department of Pharmacology & Neuroscience, 3500 Camp Bowie Blvd, University of North Texas Health Science Center, Fort Worth, TX 76107, USA. jsimpkin@hsc.unt.edu
Yang
Shao-Hua
SH
Liu
Ran
R
Perez
Evelyn
E
Cai
Zu Yun
ZY
Covey
Douglas F
DF
Green
Pattie S
PS
D000818:Animals; D004195:Disease Models, Animal; D045166:Estradiol Congeners / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D018696:Neuroprotective Agents / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D011960:Receptors, Estrogen; D015427:Reperfusion Injury / Q000188:drug therapy*; D020521:Stroke / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D045166:Estradiol Congeners; D018696:Neuroprotective Agents; D011960:Receptors, Estrogen