(-)-Cephaeline (dihydrochloride)

(-)-Cephaeline dihydrochloride is an enantiomer of Cephaeline dihydrochloride. Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with IC₅₀ of 121 μM. IC50 & Target: IC50: 121 μM (CYP2D6)^[1]
Ki: 54 μM (CYP2D6)^[1] In Vitro: 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. IC₅₀ 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_is of 54 and 355 μM for CYP2D6 and CYP3A4, respectively^[1].