- 生物活性
DPN (Diarylpropionitrile) 是一种非甾体雌激素受体 ERβ 选择性配体，其 EC50 值为 0.85 nM。DPN 在许多神经系统疾病具有神经保护作用。
- 靶点
ERβ
0.85 nM (EC
50
)
- 体外研究
DPN has a 70-fold ERα relative binding affinity selectivity, and it is a full ERα agonist with a 78-fold ERα potency selectivity (EC
50
=0.85 nM for ERβ; EC
50
=66 nM for ERα).
DPN (10 nM) prevents morphological alterations from Aβ
1-42
(10 μM)-induced toxicity in cultured cortical neurons.
DPN (0.1-100 nM) decreases ROS levels in a non-dose response manner.
DPN (0.1-100 nM) significantly reduces Aβ
1-42
-stimulated expression of Bax in a non-dose dependent manner.
DPN (0.1-100 nM) reduces activated IL-1 levels induced by Aβ
1-42
treatment on cultured cortical neurons.
DPN (0.1-100 nM) suppresses the Aβ
1-42
-upregulated phosphorylation of JNK and p38.
- 体内研究
DPN (10 μg; s.c.; daily; for 11 days) increases swimming and decreases immobility in the FST, and increases TPH protein expression in the dorsal raphe nucleus (DR) in rat model.
Animal Model:
Adult Sprague-Dawley female rats (220-250 g), ovariectomized animal models
Dosage:
10 μg/rat
Administration:
Subcutaneous injections, daily, for 11 days
Result:
Increased swimming and decreased immobility in the FST.
