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

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  • KOBAYASHI Yasuna
    Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
  • SUZUKI Michiya
    Biochemical Toxicology, School of Pharmaceutical Sciences, Showa University
  • OHSHIRO Naomi
    Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
  • SUNAGAWA Takashi
    Biochemical Toxicology, School of Pharmaceutical Sciences, Showa University
  • SASAKI Tadanori
    Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
  • TOKUYAMA Shogo
    Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
  • YAMAMOTO Toshinori
    Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
  • YOSHIDA Takemi
    Biochemical Toxicology, School of Pharmaceutical Sciences, Showa University

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We examined the effect of climbazole on the induction of rat hepatic microsomal cytochrome P450 (P450), and compared the induction potency with other N-substituted azole drugs such as clorimazole. We found that climbazole is found to be a potent inducer of rat hepatic microsomal P450 as clorimazole. Induced level of P450 by climbazole was almost similar in extent to clorimazole when compared with other imidazole drugs in a dose- and time-dependent manner. Parallel to the increase in P450, climbazole increased aminopyrine and erythromycin N-demethylase, ethoxycoumarin O-deethylase, and androstenedione 16β- and 15α/6β hydroxylase activities; however, clorimazole did not induce aminopyrine N-demethylase activity irrespective of its marked increase in P450 content. Immunoblot analyses revealed that climbazole induced CYP2B1, 3A2 and 4A1. The present findings indicate that climbazole is a new potent inducer of hepatic microsomal P450 and drug-metabolizing enzymes like clorimazole, but it may have some differential mechanism(s) for these enzymes’ induction in rat liver.

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