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驱虫药吩噻嗪在人体内的代谢情况

Fate of the anthelmintic, phenothiazine, in man.

作者信息

Mitchell S C, Kestell P, Steventon G B, Waring R H

机构信息

Biological Chemistry, Division of Biomedical Sciences, Faculty of Medicine, Imperial College, South Kensington, London SW7 2AZ, UK.

出版信息

Xenobiotica. 2002 Sep;32(9):771-82. doi: 10.1080/00498250210143038.

DOI:10.1080/00498250210143038
PMID:12396274
Abstract
  1. Radiolabelled [(35)S]-phenothiazine has been administered orally to two healthy adult male volunteers (6 mg kg(-1) body weight). Faeces were the major route of excretion of radioactivity (68%), the remainder being eliminated via the urine (32%) with an estimated urinary half-life (biphasic) of 6-16 h. Over the 5 days of the study a complete recovery of radioactivity was achieved. 2. From urinary data, it was shown that metabolism occurred via ring carbon oxidation to form phenothiazone and thionol and via ring sulphur oxidation to form phenothiazine sulphoxide. The majority of urinary material (92%) was present in the form of conjugates of phenothiazine and phenothiazone. Only unchanged phenothiazine was detected in the faeces. Phenothiazine sulphoxide was reduced to phenothiazine during incubation with faecal homogenates.
摘要
  1. 已给两名健康成年男性志愿者口服放射性标记的[(35)S] - 吩噻嗪(6毫克/千克体重)。粪便为放射性物质排泄的主要途径(68%),其余通过尿液排出(32%),估计尿液半衰期(双相)为6 - 16小时。在研究的5天内实现了放射性的完全回收。2. 从尿液数据可知,代谢通过环碳氧化形成吩噻嗪酮和硫代酚,以及通过环硫氧化形成吩噻嗪亚砜。大部分尿液物质(92%)以吩噻嗪和吩噻嗪酮的结合物形式存在。粪便中仅检测到未变化的吩噻嗪。在与粪便匀浆孵育期间,吩噻嗪亚砜被还原为吩噻嗪。

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