Ignatov Iu D, Vislobokov A I, Tiurenkov I N, Bagmetova V V
Eksp Klin Farmakol. 2012;75(12):3-6.
The new glutamic acid derivative RGPU-135 (3-phenylglutamic acid hydrochloride, glutaron, neuroglutamin) produces dose-dependent and reversible modulation of transmembrane sodium, potassium and, to a greater extent, calcium ion currents in neurons of Lymnaea stagnalis and Planorbarius corneus mollusks at concentrations of 1, 10, 100, and 1000 microM. At concentrations within 1 - 10 microM micromole, Ca and K currents are activated rather insignificantly; at 100 pmole, the amplitude of calcium currents is increased by 5 - 10%; and at 1000 microM, the Na and K ion currents are suppressed by 5 - 12%. RGPU-135 does not influence the membrane surface charge potential and the gating of ion channels. The effects of RGPU-135 were quickly reversible, which indicated the relatively weak drug binding to the membrane structures and ion channels.
新型谷氨酸衍生物RGPU - 135(3 - 苯基谷氨酸盐酸盐、戊二醛、神经谷氨酰胺)在浓度为1、10、100和1000微摩尔时,对椎实螺和角豆螺神经元中的跨膜钠、钾离子电流,以及在更大程度上对钙离子电流产生剂量依赖性且可逆的调节作用。在1 - 10微摩尔浓度范围内,钙电流和钾电流的激活作用相当不明显;在100皮摩尔时,钙电流幅度增加5 - 10%;而在1000微摩尔时,钠电流和钾电流被抑制5 - 12%。RGPU - 135不影响膜表面电荷电位和离子通道的门控。RGPU - 135的作用可快速逆转,这表明药物与膜结构和离子通道的结合相对较弱。