3,4,5-Trimethoxyphenylacetaldehyde, an Intermediate Metabolite of Mescaline, Is a Substrate for Microsomal Aldehyde Oxygenase in the Mouse Liver.
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3, 4, 5-Trimethoxyphenylacetaldehyde, an intermediate metabolite of mescaline, was oxidized to 3, 4, 5-trimethoxyphenylacetic acid by mouse hepatic microsomes. The reaction was NADPH-dependent, and inhibited by SKF 525-A, metyrapone and disulfiram. A P450 isozyme in mouse hepatic microsomes, P450 MUT-2 (CYP2C29), catalyzed the reaction (0.96 nmol/min/nmol P450) in which NADPH and NADPH-cytochrome c reductase were essential for the catalytic activity. The reaction was confirmed to be an oxygenation since molecular oxygen was incorporated into the carboxylic acid metabolite formed under oxygen-18 gas by GC-MS analysis. By addition of antibody against CYP2C29 to the microsomes (3.2 mg/mg microsomal protein) the MALDO activity was inhibited by 35% of the control value with preimmune serum, suggesting that CYP2C29 or an immunologically-related isozyme (s) plays a major role in the NADPH-dependent oxidation of 3, 4, 5-trimethoxyphenylacetaldehyde to 3, 4, 5-trimethoxyphenylacetic acid by mouse hepatic microsomes. Pharmacological experiments on mescaline and its deaminated metabolites using mice indicated that the metobolites were much less active or were inactive in cataleptogenic effect and pentobarbital-induced sleep prolongation as compared with the parent compound.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 18 (5), 696-699, 1995
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
- 1390282679600449408
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- NII論文ID
- 110003640912
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- NII書誌ID
- AA10885497
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- ISSN
- 13475215
- 09186158
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- PubMed
- 7492985
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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
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- PubMed
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