書誌事項
- タイトル別名
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- Studies on the Metabolic Fate of a Novel Orally Active Nonpeptide Endothelin Antagonist TA-0201: Metabolism and First-pass Metabolism of TA-0201 in Rats.
- 公開日
- 1998
- DOI
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- 10.2133/dmpk.13.546
- 公開者
- 日本薬物動態学会
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説明
TA-0201 is a novel orally active non-peptide antagonist for endothelin receptors. Metabolism and pharmacokinetics of TA-0201 were investigated in rat. Animal and human liver microsomes were used to investigate the metabolism of TA-0201 in vitro.<BR> 1. The structures of main metabolites were identified to be carboxylic acid form (CA) and diol form (Diol) by comparison with authentic sample using LC/MS/MS. Intrinsic clearances (CLint) for the conversion of TA-0201 to CA by liver microsomes of different species were in the following order of monkey>>dog>human>rat. The isozyme catalyzing the metabolic reaction of TA-0201 to CA and Diol was determined. It was supposed that CYP3A family contributed mainly to these metabolic reactions.<BR> 2. Pharmacokinetic studies of TA-0201 in the rat were investigated, the bioavailability (BA) in male rats was calculated as 60%. More than 90% of TA-0201 was disappeared from the body by metabolism. Hepatic and gastro intestinal extractions were 0.21 and 0.11, respectively. Contributions of the two organs in the first-pass extraction of TA-0201 after oral administration were of the same degree.
収録刊行物
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- 薬物動態
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薬物動態 13 (6), 546-556, 1998
日本薬物動態学会
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詳細情報 詳細情報について
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- CRID
- 1390282679645167232
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- NII論文ID
- 10008199030
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- NII書誌ID
- AN10144117
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- ISSN
- 09161139
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- 本文言語コード
- ja
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- データソース種別
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- JaLC
- Crossref
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可
