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二氧戊环对鼻腔和肝脏细胞色素P-450单加氧酶的抑制作用。

Inhibition of nasal and liver cytochrome P-450 mono-oxygenases by dioxolanes.

作者信息

Petridou-Fischer J, Dahl A

机构信息

Inhalation Toxicology Research Institute, Lovelace Biomedical and Environmental Research Institute, Albuquerque, NM 87185.

出版信息

Xenobiotica. 1988 Jan;18(1):1-9. doi: 10.3109/00498258809055131.

DOI:10.3109/00498258809055131
PMID:3354225
Abstract
  1. A series of six alkyl-substituted dioxolanes were studied for their inhibitory effects on mono-oxygenase activities in vitro with nasal and hepatic microsomes from rats and rabbits. 2. Carbon monoxide binding and hexamethylphosphoramide (HMPA) N-demethylase activity were most susceptible to inhibition by the test compounds. 3. Inhibition of HMPA N-demethylase activity in both nasal and liver microsomes increased with lipophilicity of the inhibiting compound. In olfactory mucosa, the bulk of the substituent at the 4-position also seemed to have an effect on inhibition. 4. Mono-oxygenase activity in the nasal mucosa was inhibited more readily than that in the liver.
摘要
  1. 研究了一系列六种烷基取代的二氧戊环对大鼠和家兔鼻腔及肝脏微粒体中单加氧酶活性的体外抑制作用。2. 一氧化碳结合及六甲基磷酰胺(HMPA)N-脱甲基酶活性对受试化合物的抑制最为敏感。3. 鼻腔和肝脏微粒体中HMPA N-脱甲基酶活性的抑制作用随抑制性化合物的亲脂性增加而增强。在嗅黏膜中,4位取代基的大小似乎也对抑制作用有影响。4. 鼻腔黏膜中的单加氧酶活性比肝脏中的更容易受到抑制。

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