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 pote...

Full description

Saved in:
Bibliographic Details
Published in:Stroke (1970) 2004-11, Vol.35 (11 Suppl 1), p.2648-2651
Main Authors: Simpkins, James W, Yang, Shao-Hua, Liu, Ran, Perez, Evelyn, Cai, Zu Yun, Covey, Douglas F, Green, Pattie S
Format: Article
Language:English
Subjects:
Animals
Disease Models, Animal
Estradiol Congeners - chemistry
Estradiol Congeners - pharmacology
Estradiol Congeners - therapeutic use
Humans
Neuroprotective Agents - pharmacology
Neuroprotective Agents - therapeutic use
Rats
Receptors, Estrogen
Reperfusion Injury - drug therapy
Stroke - drug therapy
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0039-2499
1524-4628
DOI:10.1161/01.str.0000143734.59507.88