Table 3

Correlation coefficients between nicotine N-glucuronidation, cotinine N-glucuronidation, and other glucuronidation activities in liver microsomes from 14 livers

Substrate (Conc.)Cotinine (0.2 mM)Estradiol3-a (0.1 mM)Trifluoperazine3-a (0.1 mM)Imipramine (0.5 mM)Propofol3-a (30 μM)
Nicotine (50 μM)0.9503-160 −0.3510.1990.4250.225
Cotinine (0.2 mM)−0.5310.1980.5170.227
Estradiol (0.1 mM)0.2670.1820.281
Trifluoperazine (0.1 mM)0.8163-150 0.346
Imipramine (0.5 mM)0.408

Nicotine, cotinine, or imipramine N-glucuronidations in liver microsomes from 14 humans were determined in the present study. Estradiol and propofol are typical substrates for UGT1A1 and UGT1A9, respectively. Trifluoperadine and imipramine are typical substrates for UGT1A4.

  • 3-150P < 0.005,

  • 3-160P < 0.0001.

  • 3-a  Glucuronosyltransferase activities of estradiol, trifluoperadine, and propofol in liver microsomes from 11 humans were provided by the manufacturer.