Ameri A
Department of Pharmacy and Pharmacology of Natural Compounds, University of Ulm, Germany.
Eur J Pharmacol. 1997 Sep 24;335(2-3):145-52. doi: 10.1016/s0014-2999(97)01205-3.
The effects of the two structurally related Aconitum alkaloids, 1-benzoylnapelline and napelline, were investigated by extracellular recording of the stimulus-evoked population spike in the CA1 region of rat hippocampal slices in vitro. 1-Benzoylnapelline (1-100 microM) exerted a depressant action on the orthodromic as well as on the antidromic population spike. Napelline failed to evoke a significant effect at concentrations up to 100 microM. The inhibitory action induced by 1-benzoylnapelline was enhanced when the frequency of electrical stimulation was increased. In contrast, reversal of the inhibitory effect was accelerated when stimulation frequency was decreased. The activity-dependent mode of action of 1-benzoylnapelline raised the question of whether the drug is effective to suppress epileptiform activity. The results obtained from experiments on epileptiform hippocampal slices revealed a reduction of the burst duration and of the number of spikes in the burst as well as attenuation of the amplitude of the population spikes. These data support the conclusion that 1-benzoylnapelline, in contrast to the structurally related compound, napelline, has an activity-dependent inhibitory action on central neurons.
通过细胞外记录体外培养的大鼠海马脑片CA1区刺激诱发的群体锋电位，研究了两种结构相关的乌头生物碱——1-苯甲酰乌头宁和乌头宁的作用。1-苯甲酰乌头宁（1-100微摩尔）对顺向和逆向群体锋电位均有抑制作用。乌头宁在浓度高达100微摩尔时未能产生显著作用。当电刺激频率增加时，1-苯甲酰乌头宁诱导的抑制作用增强。相反，当刺激频率降低时，抑制作用的逆转加速。1-苯甲酰乌头宁的活性依赖作用方式引发了该药物是否能有效抑制癫痫样活动的问题。从癫痫样海马脑片实验中获得的结果显示，爆发持续时间和爆发中峰电位数量减少，群体锋电位幅度衰减。这些数据支持以下结论：与结构相关的化合物乌头宁相比，1-苯甲酰乌头宁对中枢神经元具有活性依赖的抑制作用。
