Acute and subacute effects of miconazole nitrate on hepatic styrene oxide hydrolase and cytochrome P-450-dependent monooxygenase activities in male and female AKR/J mice

Climbazole is a new potent inducer of rat hepatic cytochrome P450.

“…Currently, Vargas et al (1998) have reported that chemical structure requirements for the induction of Phase II enzymes in the intestine are markedly different from that for the liver. All of these findings (Lavrijsen et al, 1986;Franklin, 1987a, 1987b;Rodrigues et al, 1988;James, 1988;Laignelet et al, 1989;Papac and Franklin, 1988;Franklin, 1991Franklin, , 1992Franklin and Moody, 1992;Cho et al, 1995;Vargas et al, 1998) together with our reports (Matsuura et al, 1991;Kobayashi et al, 1992Kobayashi et al, , 1993Kobayashi et al, , 1994Kobayashi et al, , 1995Kobayashi et al, , 1996aKobayashi et al, , 1996bKobayashi et al, , 2000Kobayashi et al, , 2001Yoshida et al, 1995) of P450 enzymes by imidazole ring-containing compounds would need to have an aromatic substitutent at 1 position of the imidazole ring. Thus, investigation and elucidation of the structural feature of imidazole derivatives as P450 inducer and/or inhibitor are important for the prediction of human and animal toxicities.…”

Climbazole is a new potent inducer of rat hepatic cytochrome P450.

“…Currently, Vargas et al (1998) have reported that chemical structure requirements for the induction of Phase II enzymes in the intestine are markedly different from that for the liver. All of these findings (Lavrijsen et al, 1986;Franklin, 1987a, 1987b;Rodrigues et al, 1988;James, 1988;Laignelet et al, 1989;Papac and Franklin, 1988;Franklin, 1991Franklin, , 1992Franklin and Moody, 1992;Cho et al, 1995;Vargas et al, 1998) together with our reports (Matsuura et al, 1991;Kobayashi et al, 1992Kobayashi et al, , 1993Kobayashi et al, , 1994Kobayashi et al, , 1995Kobayashi et al, , 1996aKobayashi et al, , 1996bKobayashi et al, , 2000Kobayashi et al, , 2001Yoshida et al, 1995) of P450 enzymes by imidazole ring-containing compounds would need to have an aromatic substitutent at 1 position of the imidazole ring. Thus, investigation and elucidation of the structural feature of imidazole derivatives as P450 inducer and/or inhibitor are important for the prediction of human and animal toxicities.…”

Effect of 4-(4-Chlorobenzyl)pyridine on Rat Hepatic Microsomal Cytochrome P450 and Drug-Metabolizing Enzymes in Vivo and in Vitro.

“…1) Many investigators have demonstrated that N-substituted imidazole-containing drugs and chemicals, such as clotrimazole and 1-benzylimidazole, are potent inducers of rat hepatic P450 and its associated mono-oxygenase activities. [2][3][4][5][6][7][8][9] To date, we have reported that compounds substituted at the 1-or 4-position of the imidazole-and pyridine-rings, respectively, are potent inducers of rat hepatic microsomal P450 in vivo, but these chemicals markedly inhibited P450-dependent mono-oxygenase activity when added in an in vitro assay system. [10][11][12][13][14] Recently, we reported that 2,2Ј-dipyridyl ketone induces both P450 and heme oxygenase activity, whereas 2,2Ј-dipyridyl and 2,2Ј-dipyridyl amine are able to increase heme oxygenase activity with a decreasing P450 content.…”

Climbazole is a new potent inducer of rat hepatic cytochrome P450.

“…Currently, Vargas et al (1998) have reported that chemical structure requirements for the induction of Phase II enzymes in the intestine are markedly different from that for the liver. All of these findings (Lavrijsen et al, 1986;Franklin, 1987a, 1987b;Rodrigues et al, 1988;James, 1988;Laignelet et al, 1989;Papac and Franklin, 1988;Franklin, 1991Franklin, , 1992Franklin and Moody, 1992;Cho et al, 1995;Vargas et al, 1998) together with our reports (Matsuura et al, 1991;Kobayashi et al, 1992Kobayashi et al, , 1993Kobayashi et al, , 1994Kobayashi et al, , 1995Kobayashi et al, , 1996aKobayashi et al, , 1996bKobayashi et al, , 2000Kobayashi et al, , 2001Yoshida et al, 1995) of P450 enzymes by imidazole ring-containing compounds would need to have an aromatic substitutent at 1 position of the imidazole ring. Thus, investigation and elucidation of the structural feature of imidazole derivatives as P450 inducer and/or inhibitor are important for the prediction of human and animal toxicities.…”

Effect of 4-(4-Chlorobenzyl)pyridine on Rat Hepatic Microsomal Cytochrome P450 and Drug-Metabolizing Enzymes in Vivo and in Vitro.

“…1) Many investigators have demonstrated that N-substituted imidazole-containing drugs and chemicals, such as clotrimazole and 1-benzylimidazole, are potent inducers of rat hepatic P450 and its associated mono-oxygenase activities. [2][3][4][5][6][7][8][9] To date, we have reported that compounds substituted at the 1-or 4-position of the imidazole-and pyridine-rings, respectively, are potent inducers of rat hepatic microsomal P450 in vivo, but these chemicals markedly inhibited P450-dependent mono-oxygenase activity when added in an in vitro assay system. [10][11][12][13][14] Recently, we reported that 2,2Ј-dipyridyl ketone induces both P450 and heme oxygenase activity, whereas 2,2Ј-dipyridyl and 2,2Ј-dipyridyl amine are able to increase heme oxygenase activity with a decreasing P450 content.…”

Climbazole is a new potent inducer of rat hepatic cytochrome P450.

“…Currently, Vargas et al (1998) have reported that chemical structure requirements for the induction of Phase II enzymes in the intestine are markedly different from that for the liver. All of these findings (Lavrijsen et al, 1986;Franklin, 1987a, 1987b;Rodrigues et al, 1988;James, 1988;Laignelet et al, 1989;Papac and Franklin, 1988;Franklin, 1991Franklin, , 1992Franklin and Moody, 1992;Cho et al, 1995;Vargas et al, 1998) together with our reports (Matsuura et al, 1991;Kobayashi et al, 1992Kobayashi et al, , 1993Kobayashi et al, , 1994Kobayashi et al, , 1995Kobayashi et al, , 1996aKobayashi et al, , 1996bKobayashi et al, , 2000Kobayashi et al, , 2001Yoshida et al, 1995) of P450 enzymes by imidazole ring-containing compounds would need to have an aromatic substitutent at 1 position of the imidazole ring. Thus, investigation and elucidation of the structural feature of imidazole derivatives as P450 inducer and/or inhibitor are important for the prediction of human and animal toxicities.…”

Effect of 4-(4-Chlorobenzyl)pyridine on Rat Hepatic Microsomal Cytochrome P450 and Drug-Metabolizing Enzymes in Vivo and in Vitro.

“…1) Many investigators have demonstrated that N-substituted imidazole-containing drugs and chemicals, such as clotrimazole and 1-benzylimidazole, are potent inducers of rat hepatic P450 and its associated mono-oxygenase activities. [2][3][4][5][6][7][8][9] To date, we have reported that compounds substituted at the 1-or 4-position of the imidazole-and pyridine-rings, respectively, are potent inducers of rat hepatic microsomal P450 in vivo, but these chemicals markedly inhibited P450-dependent mono-oxygenase activity when added in an in vitro assay system. [10][11][12][13][14] Recently, we reported that 2,2Ј-dipyridyl ketone induces both P450 and heme oxygenase activity, whereas 2,2Ј-dipyridyl and 2,2Ј-dipyridyl amine are able to increase heme oxygenase activity with a decreasing P450 content.…”