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多虑平-doxepin
变量_单倍型
CYP2D6 poor metabolizers
记事
Three human liver samples were tested for dextromethorphan o-demethylation activity as marker for CYP2D6 activity. Based on this 2 liver samples showed extensive metabolizer status (CYP2D6 activity 1.21 and 1.27 nmol/min/nmolP450), while one sample poor metabolizer status (CYP2D6 activity 0.03 nmol/min/nmolP450). Km was 6-9.6 microM for EM samples for E-doxepin. The PM sample had a similar Km value but only produced a small amount of E-hydroxydoxepin with less than one-tenth of Vmax of the EM samples. Studies with the CYP2D6 inhibitor quinidine suggests that CYP2D6 is catalyzing E-doxepin hydroxylation.
专家论述
CYP2D6 poor metabolizers are associated with decreased metabolism of doxepin in human liver microsomes as compared to CYP2D6 normal metabolizers.