Saano V, Urtti A
Pharmacol Biochem Behav. 1982 Aug;17(2):367-9. doi: 10.1016/0091-3057(82)90094-6.
Tofizopam, a 3,4-benzodiazepine, lacks the sedative action common to 1,4-benzodiazepines, but has anxiolytic activity. In this study we administered tofizopam (50 mg/kg) to rats perorally twice a day for six days, and analyzed the binding of [3H]flunitrazepam to benzodiazepine receptors of these drug-treated rats. The effect of tofizopam treatment was compared to that brought about by treatment with diazepam (12 mg/kg twice a day for six days) and to binding in controls treated with vehicle. Compared to the controls, the diazepam group had a marked decrease in binding of [3H]flunitrazepam to benzodiazepine receptors both in the forebrain and in the hindbrain. As a result of the increased affinity of the receptors tofizopam slightly, but statistically significantly, enhanced binding. With both drugs the number of receptors was unaltered. The effect of tofizopam in the hindbrain was similar to that in the forebrain. The results of this study support our earlier finding from single-dose studies that tofizopam acts indirectly on benzodiazepine receptors.
托非唑泮是一种3,4 - 苯二氮䓬类药物，缺乏1,4 - 苯二氮䓬类药物常见的镇静作用，但具有抗焦虑活性。在本研究中，我们每天给大鼠口服托非唑泮（50毫克/千克），持续六天，每天两次，并分析了这些经药物处理的大鼠中[3H]氟硝西泮与苯二氮䓬受体的结合情况。将托非唑泮治疗的效果与地西泮治疗（每天两次，每次12毫克/千克，持续六天）的效果以及用赋形剂处理的对照组的结合情况进行了比较。与对照组相比，地西泮组在前脑和后脑[3H]氟硝西泮与苯二氮䓬受体的结合均显著减少。由于受体对托非唑泮的亲和力增加，结合略有增强，但具有统计学意义。两种药物处理后受体数量均未改变。托非唑泮在后脑的作用与在前脑相似。本研究结果支持我们早期单剂量研究的发现，即托非唑泮间接作用于苯二氮䓬受体。
