Metabolism Reactions | P450 Isoform | Regression Coefficient (r2) | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
Metabolite Formationa | Overall Buspirone Metabolismb | |||||||||||
1-PP | 3′-OH | 6′-OH | 5-OH | N-oxide | ||||||||
7-Ethoxyresorufin O-dealkylation | 1A2 | 0.06 | 0.09 | 0.07 | 0.12 | 0.09 | 0.09 | |||||
Coumarin 7-hydroxylation | 2A6 | 0.25 | 0.25 | 0.24 | 0.21 | 0.18 | 0.01 | |||||
S-Mephenytoin N-demethylation | 2B6 | 0.41 | 0.32 | 0.50 | 0.32 | 0.49 | 0.40 | |||||
Diclofenac 4′-hydroxylation | 2C9 | 0.10 | 0.10 | 0.09 | 0.11 | 0.06 | 0.03 | |||||
S-Mephenytoin 4′-hydroxylation | 2C19 | 0.36 | 0.32 | 0.31 | 0.28 | 0.44 | 0.35 | |||||
Dextromethorphan O-demethylation | 2D6 | 0.08 | 0.08 | 0.08 | 0.06 | 0.09 | 0.11 | |||||
Chlorzoxazone 6-hydroxylation | 2E1 | 0.08 | 0.12 | 0.08 | 0.09 | 0.09 | 0.13 | |||||
Testosterone 6β-hydroxylation | 3A4 | 0.96*** | 0.92*** | 0.93*** | 0.85*** | 0.86*** | 0.92*** |
↵ a Data presented in this table were averaged from analyses of duplicate incubations. Statistical significance of the correlation between metabolism rates and P450 enzyme activities is denoted by ***ρ <0.0005
↵ b The rate of the overall metabolism was calculated based on the conversion of buspirone to the total metabolite peaks