Bondarenko N A, Gorantcheva J, Tyutyulkova N, Nikolova M, Valdman A V
Chemical Pharmaceutical Research Institute, Sofia, Bulgaria.
Methods Find Exp Clin Pharmacol. 1988 Oct;10(10):629-33.
The effects of a new benzamide derivative LIS-630 and the well-known neuroleptic, tiapride, were studied on stress-induced hyper- and hypoactive emotional behavioral reaction of animals depending on the individual ability for perceptive-cognitive activity in stress situations, and their affinity to striatal DA receptors. A modified variant of forced swimming method was used. The affinity of the substances to striatal DA receptors was studied by the radioligand binding method using 3H-spiroperidol. The results show that the psychopharmacological profile of LIS-630 differs significantly from the neuroleptic, tiapride. LIS-630 restored escape behavior from stress situation after preliminary exposure of rats to forced swimming and did not disturb escape behavior in animals more resistant to emotional hypoactivity. LIS-630 reduced immobility time at forced swimming. However, it is not effective in preventing hyperemotional reactions induced by L-dopa and stress. The radioligand binding study shows that LIS-630 did not displace 3H-spiroperidol from the binding sites of striatum membranes. The parameters of displacement with tiapride were satisfactory.
研究了新型苯甲酰胺衍生物LIS - 630和著名的抗精神病药物硫必利，对动物应激诱导的过度和低活性情绪行为反应的影响，该影响取决于动物在应激情况下的感知 - 认知活动个体能力及其对纹状体多巴胺（DA）受体的亲和力。采用了改良的强迫游泳法。使用3H - 螺哌啶醇通过放射性配体结合法研究了这些物质对纹状体DA受体的亲和力。结果表明，LIS - 630的精神药理学特征与抗精神病药物硫必利有显著差异。在大鼠预先暴露于强迫游泳后，LIS - 630恢复了其从应激状态下的逃避行为，并且不会干扰对情绪低活性更具抵抗力的动物的逃避行为。LIS - 630减少了强迫游泳时的不动时间。然而，它在预防由左旋多巴和应激诱导的过度情绪反应方面无效。放射性配体结合研究表明，LIS - 630不会从纹状体膜的结合位点上取代3H - 螺哌啶醇。硫必利的取代参数令人满意。
