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盐酸茚洛嗪的代谢命运:大鼠体内α-葡萄糖苷的形成

Metabolic fate of indeloxazine hydrochloride: alpha-glucoside formation in rats.

作者信息

Kamimura H, Kawai R, Kudo H

机构信息

Drug Metabolism Department, Yamanouchi Pharmaceutical Co., Ltd, Tokyo, Japan.

出版信息

Xenobiotica. 1988 Feb;18(2):141-9. doi: 10.3109/00498258809041650.

DOI:10.3109/00498258809041650
PMID:3287777
Abstract
  1. After oral administration of indeloxazine hydrochloride ((+/-)-2-[(inden-7-yloxy)methyl]morpholine hydrochloride) to rats, two conjugates, which were labile to alpha-glucosidase hydrolysis but refractory to beta-glucosidase, were isolated from the urine. 2. Mass spectral and n.m.r. analyses confirmed that these conjugates were alpha-D-glucopyranosides of M-2 (trans-4-(2-morpholinylmethoxy)-1,2-indandiol) and M-3 (trans-6-[[(1,2-dihydroxy-4-indanyl)oxy]-methyl]-3-morpholinone). 3. These are probably the first examples of foreign compounds conjugated with glucose in the alpha-configuration.
摘要
  1. 给大鼠口服盐酸茚洛嗪((+/-)-2-[(茚-7-基氧基)甲基]吗啉盐酸盐)后,从尿液中分离出两种对α-葡萄糖苷酶水解不稳定但对β-葡萄糖苷酶稳定的缀合物。2. 质谱和核磁共振分析证实这些缀合物是M-2(反式-4-(2-吗啉基甲氧基)-1,2-茚二醇)和M-3(反式-6-[[(1,2-二羟基-4-茚基)氧基]甲基]-3-吗啉酮)的α-D-吡喃葡萄糖苷。3. 这些可能是与葡萄糖以α-构型缀合的外来化合物的首个实例。

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