Wildmann J, Möhler H, Vetter W, Ranalder U, Schmidt K, Maurer R
Pharmaceutical Department, F. Hoffmann-La Roche & Co., Ltd., Basle, Switzerland.
J Neural Transm. 1987;70(3-4):383-98. doi: 10.1007/BF01253613.
Benzodiazepine-binding inhibitory (BBI) activity was detected in aqueous extracts of brain and peripheral tissues of rats. The BBI activity in brain and in adrenals was, at least partially, due to the presence of N-desmethyldiazepam and diazepam as shown by HPLC, UV-spectroscopy and mass spectrometry. In addition, BBI activity was found in standardized rat food, as well as in a variety of cereals and in other nutritive plant products. In wheat grains diazepam and N-desmethyldiazepam could be identified by HPLC and analysis by gas chromatography combined with mass spectrometry. The estimated amounts of the two benzodiazepines present in rat brain and adrenals and in wheat grains were in the low ppb range. Since laboratory contamination was rigorously excluded we conclude that diazepam and N-desmethyldiazepam are naturally occurring compounds. These findings may explain their occurrence in the brain and adrenals of animals.
在大鼠的脑和外周组织水提取物中检测到苯二氮䓬结合抑制(BBI)活性。高效液相色谱(HPLC)、紫外光谱和质谱分析表明,脑和肾上腺中的BBI活性至少部分归因于N-去甲基地西泮和地西泮的存在。此外,在标准化大鼠食物、多种谷物和其他营养植物产品中也发现了BBI活性。通过HPLC以及气相色谱-质谱联用分析,在小麦籽粒中可鉴定出地西泮和N-去甲基地西泮。大鼠脑、肾上腺和小麦籽粒中这两种苯二氮䓬的估计含量处于低ppb范围。由于已严格排除实验室污染,我们得出结论,地西泮和N-去甲基地西泮是天然存在的化合物。这些发现可能解释了它们在动物脑和肾上腺中的存在。