Gobbi M, Bergami A, Caltavuturo C, Valle F D, Mennini T, Caccia S
Istituto di Ricerche Farmacologiche-Mario Negti, Milano, Italy.
Neurosci Lett. 1996 Nov 15;219(1):5-8. doi: 10.1016/s0304-3940(96)13160-8.
The effects of oral dexnorfenfluramine (DNF; 1-4 mg/kg, twice daily for 4 days), the active metabolite of dexfenfluramine, were examined on rat regional brain indole contents and [3H]citalopram binding. Two hours after the last dose, serotonin (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) were dose-dependently lowered at doses above 1.5 mg/kg, with slight regional differences. Cortical 5-HT uptake sites were reduced only at the highest dose. Above 2 mg/kg DNF also caused a more lasting reduction (4 weeks) of regional indoles and cortical 5-HT uptake sites. At this longer time while the decrease in hippocampal 5-HT levels and cortical 5-HT uptake sites remained essentially constant, cortical and striatal 5-HT levels were lowered less than at 2 h, suggesting a return toward control values.
研究了右芬氟拉明的活性代谢物口服右诺氟拉明（DNF；1 - 4毫克/千克，每日两次，共4天）对大鼠脑区吲哚含量和[³H]西酞普兰结合的影响。末次给药后两小时，剂量高于1.5毫克/千克时，血清素（5 - HT）和5 - 羟吲哚乙酸（5 - HIAA）呈剂量依赖性降低，存在轻微的区域差异。仅在最高剂量时皮质5 - HT摄取位点减少。高于2毫克/千克的DNF还导致区域吲哚和皮质5 - HT摄取位点更持久的减少（4周）。在这个较长时间，海马体5 - HT水平和皮质5 - HT摄取位点的降低基本保持不变，而皮质和纹状体5 - HT水平的降低程度低于2小时时，表明其向对照值恢复。
