Moroi K, Kuga T
Jpn J Pharmacol. 1987 Jan;43(1):33-41. doi: 10.1254/jjp.43.33.
Brain harmine was simply and sensitively determined by high performance liquid chromatography (HPLC), and the relationship between brain harmine concentrations and the jumping behavior induced by harmine and apomorphine was investigated. The concentration of harmine and the peak height in HPLC showed a good correlation, and the detection limit was 0.05 pmole harmine. In rats treated with 2, 5 and 10 mg/kg of harmine, the concentrations of harmine in the brain cortex were 9.0, 21.3 and 43.1 nmole/g tissue (wet wt.), respectively. The regional brain harmine concentrations and the jumping activity measuring by a scoring system increased with increasing doses of harmine administered, and there was a direct relation between the harmine concentrations and the jumping activity. This relation was observed in washed membranes in which about 40% of the harmine in whole homogenate was present. Tissue subfractionation showed that 30% of the harmine in whole brain homogenates was in the P2 fraction, and of this, 70% was located in the synaptosomes. The brain homogenate did not metabolize harmine and no metabolite was detected in the brain 10 min after treatment with harmine and apomorphine. These results suggest that harmine itself, but not its metabolites, may be responsible for inducing the jumping behavior and that the jumping activity is correlated with brain harmine concentrations.
采用高效液相色谱法（HPLC）简单灵敏地测定了脑内去氢骆驼蓬碱，并研究了脑内去氢骆驼蓬碱浓度与去氢骆驼蓬碱和阿扑吗啡诱导的跳跃行为之间的关系。去氢骆驼蓬碱浓度与HPLC中的峰高显示出良好的相关性，检测限为0.05皮摩尔去氢骆驼蓬碱。在用2、5和10mg/kg去氢骆驼蓬碱处理的大鼠中，大脑皮层中去氢骆驼蓬碱的浓度分别为9.0、21.3和43.1纳摩尔/克组织（湿重）。通过评分系统测量的脑内区域去氢骆驼蓬碱浓度和跳跃活动随着给予去氢骆驼蓬碱剂量的增加而增加，并且去氢骆驼蓬碱浓度与跳跃活动之间存在直接关系。在洗涤过的膜中观察到这种关系，在整个匀浆中约40%的去氢骆驼蓬碱存在于其中。组织分级分离表明，全脑匀浆中30%的去氢骆驼蓬碱存在于P2组分中，其中70%位于突触体中。脑匀浆不代谢去氢骆驼蓬碱，在用去氢骆驼蓬碱和阿扑吗啡处理10分钟后，脑中未检测到代谢产物。这些结果表明，去氢骆驼蓬碱本身而非其代谢产物可能是诱导跳跃行为的原因，并且跳跃活动与脑内去氢骆驼蓬碱浓度相关。
