Metabolism of Cloxazolam. I. Distribution, Excretion and Biotransformation in Rats and Mice
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- MURATA HISASHI
- Central Research Laboratories, Sankyo Co., Ltd.
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- KOUGO KATSUMI
- Central Research Laboratories, Sankyo Co., Ltd.
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- YASUMURA AKIRA
- Central Research Laboratories, Sankyo Co., Ltd.
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- NAKAJIMA EIICHI
- Central Research Laboratories, Sankyo Co., Ltd.
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- SHINDO HIDEYO
- Central Research Laboratories, Sankyo Co., Ltd.
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The distribution, excretion and biotransformation of 14C-cloxazolam were studied in rats and mice. The tissue concentration reached the maximum at about 1 and 3 hr after oral administration to rats and mice, respectively. The brain concentration was higher and lasted longer in mice than in rats. In the whole-body autoradiograms of mice, no significant radioactivity was detected in the tissues except the liver after 24 hr and the radioactivity disappeared almost completely after 72 hr. The recovery of radioactivity was considerably higher in the feces than in the urine and was about the same regardless of the route of administration in both rats and mice. In the in situ cannulated rats, the most of the oral dose was recovered in the bile in 24 hr period. Eighteen radioactive metabolites were detected in the liver, urine and feces after oral administration of 14C-cloxazolam. Among them, eight metabolites including 7-chloro-2, 3-dihydro-5-[o-chlorophenyl]-2H-1, 4-benzodiazepin-2-one, 7-chloro-5-[o-chlorophenyl]-1, 3-dihydro-3-hydroxy-2H-1, 4-benzodiazepin-2-one (COX) and 2-amino-3-hydroxy-2', 5-dichlorobenzophenone (ADCB-OH) were isolated and identified. The main metabolites in the mouse urine were the glucuronides of COX and ADCB-OH, while in the rat urine two unidentified metabolites in addition to the above two. In the mouse feces, COX and ADCB-OH and their conjugates were the main metabolites, while in the rat feces a much larger number of metabolites were detected.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 21 (2), 404-414, 1973
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679148582912
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- NII論文ID
- 110003661968
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- PubMed
- 4753311
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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
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可