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Guanfu base A

CAS No. : 1394-48-5

MCE 国际站：Guanfu base A

产品活性：Guanfu base A 是一种从 Aconitum coreanum 中分离的抗心律失常的生物碱，是一种有效的非竞争性 CYP2D6 抑制剂，对人肝微粒体 (HLM) 的 K_i 为 1.20 μM，对人重组体 (rCYP2D6) 的 K_i 为 0.37 μM。Guanfu base A 也是 CYP2D 的有效竞争抑制剂，对猴子和狗的微粒体的 K_i 分别为 0.38 μM，2.4 μM。Guanfu base A 还能抑制 HERG 通道电流。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

结构分类：生物碱

来源：植物  |  毛茛科  |  乌头

In Vitro: Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant CYP1A2, 2A6, 2C8, 2C19, 3A4, or 3A5, but shows slight inhibition of 2B6 and 2E1.
Guanfu base A is a potent inhibitor of CYP2D6, with an IC₅₀ recorded at ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM).
The effects of Guanfu base A is investigated in human embryonic kidney 293 (HEK293) cells transiently transfected with HERG complementary DNA using a whole-cell patch clamp technique. Guanfu base A inhibits HERG channel current in concentration-, voltage-, and time-dependent manners with an IC₅₀ of 1.64 mM. Guanfu base A shifts the activation curve in a negative direction and accelerated channel inactivation but shows no effect on the inactivation curve.

In Vivo: Beagle dogs treated intravenously with Dextromethorphan (2 mg/mL) after pretreatment with Guanfu base A injection shows reduced CYP2D metabolic activity, with the C_max of dextrorphan being one-third that of the saline-treated group and area under the plasma concentration-time curve half that of the saline-treated group.

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