TABLE 3

Propofol inhibition of HLM-catalyzed N-glucuronidation

Rates were determined for each substrate in duplicate in the presence or absence of 100 μM propofol. Duplicates agreed within 10%.


Sample

Percentage Inhibition of N-Glucuronidation
Imipraminea (pH 8.9)
Nicotineb
Cotininec
pH 7.1
pH 8.9
pH 7.1
pH 8.9
109 9 16 4 70 35
127 6 45 3 58 18
130 0 32 6 64 41
132 5 30 17 61 32
133 0 16 27 64 42
134
3
25
24
66
42
  • a 1 mM imipramine and 2 mM UDPGA.

  • b 5 mM nicotine and 2 mM [14C]UDPGA (1-2 nCi/nmol).

  • c 5 mM cotinine and 2 mM [14C]UDPGA (0.5 nCi/nmol).