TABLE 1

TSU-68 hydroxylation by human cDNA-expressed P450 isoforms

TSU-68 (50 μM) was incubated with insect cell microsomes containing cDNA-expressed P450 isoforms in the presence of a NADPH-generating system.


cDNA-Expressed Human P450 isoform

Formation of TSU-68 Metabolite
M1
M2
M3
pmol/min/pmol P450
CYP1A1 28.8 29.1 0.57
CYP1A2 6.5 21.1 3.9
CYP2A6 a
CYP2B6
CYP2C8 0.18 0.04 0.03
CYP2C9
CYP2C19
CYP2D6 0.21
CYP2E1
CYP3A4

0.15

  • a —, not detected.