Abramets I I, Talalaenko A N, Stakhovskiĭ Iu V
Eksp Klin Farmakol. 1992 Nov-Dec;55(6):5-7.
The 1-(2-pyrimidinyl)-piperazine derivatives campirone, campironine, levopironine) evoked hyperpolarizing responses of rat dorsal root ganglion neurons mediated by 5-hydroxytryptamine(1A) receptor activation and, like chlordiazepoxide, potentiated neuronal responses evoked by GABA-depolarizing receptor activation. The drugs studied in the lighted space and threatening situation avoidance tests showed an anxiolytic effect. Picrotoxin was found to be effective in inhibiting the anxiolytic effect of chlordiazepoxide, levopironine and campironine, but it failed to affect the antianxious action of campirone. Whether the GABA-ergic mechanisms may contribute to the anxiolytic action of 1-(2-pyrimidinyl)-piperazine derivatives.
1-(2-嘧啶基)-哌嗪衍生物(坎皮酮、坎皮罗宁、左匹罗宁)可诱发大鼠背根神经节神经元的超极化反应,该反应由5-羟色胺(1A)受体激活介导,并且与氯氮卓一样,可增强由GABA去极化受体激活所诱发的神经元反应。在明场和威胁情境回避试验中研究的这些药物显示出抗焦虑作用。发现苦味毒可有效抑制氯氮卓、左匹罗宁和坎皮罗宁的抗焦虑作用,但它未能影响坎皮酮的抗焦虑作用。GABA能机制是否可能有助于1-(2-嘧啶基)-哌嗪衍生物的抗焦虑作用。