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
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- SUZUKI Michiya
- Biochemical Toxicology, School of Pharmaceutical Sciences, Showa University
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- OHSHIRO Naomi
- Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
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- SUNAGAWA Takashi
- Biochemical Toxicology, School of Pharmaceutical Sciences, Showa University
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- SASAKI Tadanori
- Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
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- TOKUYAMA Shogo
- Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
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- YAMAMOTO Toshinori
- Departments of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University
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- 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.
収録刊行物
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- The Journal of Toxicological Sciences
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The Journal of Toxicological Sciences 26 (3), 141-150, 2001
一般社団法人 日本毒性学会
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詳細情報 詳細情報について
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- CRID
- 1390282679877058048
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- NII論文ID
- 110001806915
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- NII書誌ID
- AN00002808
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- COI
- 1:CAS:528:DC%2BD3MXnsVyns78%3D
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- ISSN
- 18803989
- 03881350
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- NDL書誌ID
- 5875890
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- PubMed
- 11552297
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可