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一种涉及甲硫基连接的溴西泮新代谢途径。

A new metabolic pathway of bromazepam involving attachment of a methylthio group.

作者信息

Tateishi M, Shimizu H

出版信息

Xenobiotica. 1976 Jul;6(7):431-9. doi: 10.3109/00498257609151656.

Abstract
  1. The structures of three hitherto unidentified metabolites of bromazepam in the rat were elucidated using u.v., mass, n.m.r. and i.r. spectrometry. 2. All three metabolites contained a methylthio or corresponding oxidized group at the C-6' position of the pyridyl moiety. 3. Quantitative analysis of the metabolites determined after administration of [14C]bromazepam to rat revealed that the three metabolites together comprised about 6% of the total radioactivity excreted in the 24-h urine, or about 1% of the dose.
摘要
  1. 利用紫外光谱、质谱、核磁共振和红外光谱法阐明了大鼠体内溴西泮三种迄今未明确的代谢物的结构。2. 所有三种代谢物在吡啶基部分的C-6'位置都含有一个甲硫基或相应的氧化基团。3. 对给大鼠施用[14C]溴西泮后测定的代谢物进行定量分析表明,这三种代谢物合起来约占24小时尿液中排泄的总放射性的6%,或约占剂量的1%。

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