Physical and Chemical Properties | White to yellow powder, soluble in methanol, ethanol, DMSO and other organic solvents, derived from ipecac, angola octagonal maple. |
In vitro study | CYP2D6 reveals the highest metabolic activity for the generation of 9-O-demethylEmetine, whereas this enzyme also shows a significant metabolic activity for the generation of Cephaeline. The IC 50 s of Cephaeline against CYP2C9, CYP2D6 and CYP3A4 is over 1000, 121 and 1000 μM, respectively. Further experiments are performed to determine inhibition constants (K i ) for Cephaeline on the CYP2D6 and CYP3A4 activities Graphic analysis of Dixon plots at various Cephaeline concentrations for each of the two CYP enzyme assays yield K i s of 54 and 355 μM for CYP2D6 and CYP3A4, respectively. |