Kawaji A, Yamaguchi T, Tochino Y, Isobe M, Takabatake E
Department of Toxicology, Faculty of Pharmaceutical Sciences, Setsunan University, Hirakata, Osaka, Japan.
Biol Pharm Bull. 1999 Jan;22(1):1-4. doi: 10.1248/bpb.22.1.
N-Oxidation of benzydamine (BZY) mediated by flavin-containing monooxygenase (FMO) was evaluated by microdialysis in vivo in different regions of rat brain and liver. The probe was implanted into local regions of the brain, such as the olfactory bulb, cerebral cortex, corpus striatum, hippocampus and cerebellum, or the hepatic lobe. By perfusing BZY via the probe, BZY N-oxide was identified in the dialysate. The estimated concentrations of BZY N-oxide in extracellular fluid were almost the same as those in the olfactory bulb, hippocampus and cerebral cortex, half the concentration in the hepatic lobe; however, the concentration in the corpus striatum was lower and that in the cerebellum was higher than in the other regions. These results demonstrate that the extracellular concentration of BZY N-oxide formed in vivo was unexpectedly high in every brain region.
通过微透析法在大鼠脑和肝的不同区域体内评估了含黄素单加氧酶（FMO）介导的苄达明（BZY）的N-氧化作用。将探针植入脑的局部区域，如嗅球、大脑皮层、纹状体、海马体和小脑，或肝叶。通过探针灌注BZY后，在透析液中鉴定出了BZY N-氧化物。细胞外液中BZY N-氧化物的估计浓度在嗅球、海马体和大脑皮层中几乎相同，在肝叶中的浓度为其一半；然而，纹状体中的浓度较低，而小脑中的浓度高于其他区域。这些结果表明，体内形成的BZY N-氧化物在每个脑区的细胞外浓度出乎意料地高。
