Guan-fu base A 是一种生物碱，分离自Aconitum coreanum，是非竞争性CYP2D6抑制剂，对人肝微粒体 (HLM) 的Ki为 1.20 μM，对人重组体 (rCYP2D6) 的Ki为 0.37 μM。它也是CYP2D的有效竞争抑制剂。它还能抑制HERG通道电流。Guan-fu base A具有抗心律失常的作用。

Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.

Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant 2C8, 2C19, CYP1A2, 2A6, 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)[1]. 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 [2].

Beagle dogs treated intravenously with Dextromethorphan (2 mg/mL) after pretreatment with Guanfu base A injection shows reduced CYP2D metabolic activity, with the Cmax 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 [1].

1394-48-5

C24H31NO6

429.513

关附甲素;Guan-fu base A

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