- 生物活性
Antihistamine-1 是能够渗透血脑屏障的 H1-抗组胺药 (Ki=6.9 nM), 它也是 CYP2D6 和 hERG 通道的抑制剂,其 IC50 值分别为 5.4 和 0.8 μM。
- 靶点
CYP2D6
5.4 μM (IC
50
)
- 体外研究
Antihistamine-1 (Compound 2) is a H1-antihistamine (K
i
=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC
50
s of 5.4 and 0.8 μM, respectively.