Propylpyrazole Triol

Estrogen receptor ? (ER?) and ER? are ligand-activated transcription factors that mediate the actions of estrogen. Activation of ER?, but not ER?, is required for the cardioprotective effects of estradiol. Propylpyrazole triol (PPT) is an ER? selective agonist with a 410-fold relative binding affinity for ER? (49%) versus ER? (0.12%) and therefore activates gene transcription only through ER?.{14163,14165} In an in vivo rabbit model of ischemia-reperfusion injury, treatment with estradiol and PPT, but not diarylpropinitrile (a selective agonist of ER?) significantly decreased the infarct size compared with vehicle.{14590}