Fernándex-Tomé M P, Fuentes J A, Madroñero R, del Río J
Arzneimittelforschung. 1975 Jun;25(6):926-34.
The pharmacological actions of 6,7-tetramethylene-5-phenyl-1,2,-dihydro-3H-thieno]2,3-e](1,4)-diazepin-2-one (QM-6008, thiadiapone), a new psychotropic drug, have been studied. QM-6008 shares many of the psychosedative effects in rodents of benzodiazepines. The electroencephalographic actions in rats and rabbits of QM-6008 and chlordiazepoxide are also rather similar. This new compounds is endowed with clear conflict attenuating properties in an approach-avoidance schedule and can be considered, in consequence, as a new potentially useful anxiolytic drug. In other operant conditioning procedures in rats--Variable Interval and Discriminated Avoidance--QM-6008 induces an increase in response rate which is not generally shared by chlordiazepoxide. The psychopharmacological data collected in the present work leal to classify this new thienodiazepine derviative within the fram of tranquilizers of the benxodaizapine type. The sedative effects of QM-6008 appear howerer to be less potent and the psychostimulatn effects more markde than those ofchlordiazeposide.
一种新型精神药物6,7 - 四亚甲基 - 5 - 苯基 - 1,2 - 二氢 - 3H - 噻吩并[2,3 - e][1,4] - 二氮杂䓬 - 2 - 酮(QM - 6008,噻二氮平)的药理作用已得到研究。QM - 6008在啮齿动物中具有许多与苯二氮䓬类药物相似的精神镇静作用。QM - 6008和氯氮䓬对大鼠和兔子的脑电图作用也相当相似。这种新化合物在趋避式条件反射实验中具有明显的冲突减弱特性,因此可以被认为是一种新的潜在有用的抗焦虑药物。在大鼠的其他操作性条件反射实验——可变间隔和辨别性回避实验中——QM - 6008能使反应率增加,而氯氮䓬一般不具有这种作用。目前这项研究中收集的精神药理学数据表明,这种新的噻吩并二氮杂䓬衍生物可归类于苯并二氮杂䓬类镇静剂范畴。然而,QM - 6008的镇静作用似乎比氯氮䓬弱,而精神刺激作用比氯氮䓬更明显。