Datta R K, Ghosh J J
Naunyn Schmiedebergs Arch Pharmacol. 1977 Feb;296(3):297-300. doi: 10.1007/BF00498697.
Brain-cortex slices demethylate mescaline and p-methoxyacetanilide, a reference O-demethylating substrate, though the rate of demethylation of mescaline is about one third that of the reference substrate. The demethylase activity is localized mostly in the soluble supernatant (105 000 x g). It is purified 47-fold with respect to the demethylation of mescaline by ammonium sulfate precipitation and DEAE cellulose chromatography. The partially purified demethylase, which is stable for 3-5 days at -5 degrees C in the presence of dithiothreitol and glutathione and is inhibited by p-chloromercuribenzoate, has maximal activity at pH between 7.2 and 8.0. It demethylates mescaline into 3,4-dimethoxy-5-hydroxyphenethylamine and 3,5-dimethoxy-4-hydroxyphenethylamine and some unidentified derivatives.
脑皮质切片可使三甲氧苯乙胺和对甲氧基乙酰苯胺(一种用作参考的O-脱甲基化底物)脱甲基,不过三甲氧苯乙胺的脱甲基速率约为参考底物的三分之一。脱甲基酶活性主要定位于可溶性上清液(105000×g)中。通过硫酸铵沉淀和DEAE纤维素色谱法,相对于三甲氧苯乙胺的脱甲基作用,该酶被纯化了47倍。部分纯化的脱甲基酶在二硫苏糖醇和谷胱甘肽存在的情况下,于-5℃可稳定保存3至5天,且被对氯汞苯甲酸抑制,在pH值介于7.2至8.0之间时具有最大活性。它将三甲氧苯乙胺脱甲基生成3,4-二甲氧基-5-羟基苯乙胺和3,5-二甲氧基-4-羟基苯乙胺以及一些未鉴定的衍生物。