Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%). PPT also exerts anti-diabetic effects in mouse models.
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%). The EC50 of Propyl pyrazole triol for the ERα-dependent response is 140 pM in ERα-U2OS(human osteosarcoma)-Luc cells. In the T47D-ERbeta cell line, PPT was unable to suppress cell proliferation at all ratios of ERalpha/ERbeta expression, reflecting its ability to activate only ERalpha and not ERbeta[1]. Moreover, repeated administration of the selective oestrogen receptors (ER)α agonist propyl-pyrazole triol (PPT) results in anxiolytic-like behaviours on the elevated plus maze (EPM) in primiparous (but not nulliparous) female rats. Acute PPT administration significantly modified EPM (elevated plus maze) behaviour as a function of reproductive experience, with nulliparous females tending toward increased anxiety-like behaviours and primiparous females tending toward decreased anxiety-like behaviours[2]. The increased MPO (myeloperoxidase) levels were inhibited with PPT in male pancreas and female lung and with 17β-estradiol in female pancreas[3].
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