Coenen A M, Stephens D N, Van Luijtelaar E L
Department of Psychology, University of Nijmegen, The Netherlands.
Pharmacol Biochem Behav. 1992 Jul;42(3):401-5. doi: 10.1016/0091-3057(92)90132-y.
The profile of the anxiolytic beta-carboline isopropyl 6-benzyloxy-4-methoxymethyl beta-carboline-3-carboxylate (abecarnil; ZK 112 119), a partial agonist at benzodiazepine receptors, was determined in two experiments. In the first, abecarnil was given to WAG/Rij rats; these rats generate spontaneously occurring spike-wave discharges and are regarded as a model for absence epilepsy. Effects were measured on epileptic activity, together with those on the spectral content of the background electroencephalograph (EEG), as well as on ongoing behavior. In a second experiment, effects on sleep and behavior were investigated in Wistar rats. It was found that, similarly to classical benzodiazepines, abecarnil possessed a strong antiepileptic character and also changed the background EEG to more high-frequency waves and less spindle activity. It also produced more immobile behavior. Abecarnil induced only small, marginally significant increases in slow-wave sleep while reducing REM sleep as a proportion of total sleep. It also reduced the number of REM periods. These observations are consistent with the proposed partial agonist activity of abecarnil, a drug with interesting therapeutic implications.
在两项实验中测定了抗焦虑β-咔啉异丙基6-苄氧基-4-甲氧基甲基β-咔啉-3-羧酸酯（阿贝卡尼；ZK 112 119）的特性，它是苯二氮䓬受体的部分激动剂。在第一项实验中，将阿贝卡尼给予WAG/Rij大鼠；这些大鼠会自发产生棘波-慢波放电，被视为失神癫痫的模型。测量了其对癫痫活动的影响，以及对背景脑电图（EEG）频谱内容和正在进行的行为的影响。在第二项实验中，研究了阿贝卡尼对Wistar大鼠睡眠和行为的影响。结果发现，与经典苯二氮䓬类药物相似，阿贝卡尼具有很强的抗癫痫特性，还使背景脑电图转变为更多的高频波和更少的纺锤波活动。它还产生了更多的静止行为。阿贝卡尼仅使慢波睡眠略有增加且增加幅度不显著，同时作为总睡眠比例的快速眼动睡眠减少。它还减少了快速眼动睡眠期的数量。这些观察结果与阿贝卡尼所提出的部分激动剂活性一致，这是一种具有有趣治疗意义的药物。
