Ono H, Morishita S, Kasuya M, Kobayashi M, Miyamoto M, Oka J, Goto M, Fukuda H
Arzneimittelforschung. 1987 Apr;37(4):384-8.
(6-(7-Chloro-1,8-naphthyridin-2-yl)-7-oxo-2,3,6,7-tetrahydro-5H- 1,4- dithiino[2,3-c]pyrrol-5-yl)-4-methyl-1-piperazinecarboxylate (suriclone, RP 31264), a new anxiolytic, produced behavioral effects similar to those of diazepam and lorazepam, had a protective effect against electroshock convulsion and potentiated the sleeping effect of hexobarbital in mice. It inhibited crossed extensor reflexes in chicks and augmented the dorsal root reflex potential, the increase of which is considered to be an index of increased GABAergic presynaptic inhibition. Suriclone produced high-amplitude slow waves in the amygdala and cerebral cortex and desynchronization of theta waves in the hippocampus in rat electroencephalogram (EEG). These observations were quantitatively confirmed by power spectrum analysis of EEG. The mechanisms of action of suriclone on the CNS are discussed in relation to those of benzodiazepines.
(6-(7-氯-1,8-萘啶-2-基)-7-氧代-2,3,6,7-四氢-5H-1,4-二硫代并[2,3-c]吡咯-5-基)-4-甲基-1-哌嗪羧酸酯（舒立克隆，RP 31264）是一种新型抗焦虑药，其产生的行为效应与地西泮和劳拉西泮相似，对电休克惊厥有保护作用，并能增强小鼠戊巴比妥的催眠效果。它能抑制雏鸡的交叉伸肌反射，并增强背根反射电位，背根反射电位的增加被认为是γ-氨基丁酸能突触前抑制增强的指标。舒立克隆在大鼠脑电图（EEG）中可在杏仁核和大脑皮层产生高幅慢波，并使海马体中的θ波去同步化。这些观察结果通过脑电图的功率谱分析得到了定量证实。本文结合苯二氮䓬类药物的作用机制对舒立克隆在中枢神经系统的作用机制进行了讨论。
