DELCASTILLO J, DEMELLO W C, MORALES T
Br J Pharmacol Chemother. 1964 Jun;22(3):463-77. doi: 10.1111/j.1476-5381.1964.tb01701.x.
The effects of piperazine on Ascaris muscle cells have been investigated with electrophysiological techniques. These cells have an average resting potential of about 30 mV interrupted by rhythmic spikes of myogenic origin (1 to 7 spikes/sec). With piperazine (10(-3), w/v), the average resting potential increases above 40 mV and the pacemaker activity is suppressed. These changes are similar to those temporarily produced in the same cells by the electrical stimulation of inhibitory nerve fibres. Electrophoretic application of piperazine to different areas of the muscle cells shows that this drug hyperpolarizes their membrane only when applied to the region where both excitatory and inhibitory neuromuscular synapses are located. The degree of muscle hyperpolarization induced by piperazine depends upon the extracellular chloride concentration, decreasing when a fraction of the chloride ions is replaced by the larger, supposedly nonpenetrating, sulphate anions. Piperazine may, therefore, be regarded as a pharmacological analogue of a natural inhibitory transmitter.
已用电生理学技术研究了哌嗪对蛔虫肌细胞的作用。这些细胞的平均静息电位约为30mV,有肌源性节律性尖峰(1至7次尖峰/秒)间断。使用哌嗪(10⁻³,w/v)时,平均静息电位升至40mV以上,起搏活动受到抑制。这些变化类似于通过抑制性神经纤维电刺激在同一细胞中暂时产生的变化。将哌嗪电泳施加于肌细胞的不同区域表明,该药物仅在施加于兴奋性和抑制性神经肌肉突触均所在的区域时才使其膜超极化。哌嗪诱导的肌肉超极化程度取决于细胞外氯离子浓度,当一部分氯离子被较大的、据推测不可通透的硫酸根阴离子替代时,超极化程度降低。因此,哌嗪可被视为天然抑制性递质的药理学类似物。