Samanin R, Bendotti C, Bernasconi S, Borroni E, Garattini S
Eur J Pharmacol. 1977 May 15;43(2):117-24. doi: 10.1016/0014-2999(77)90124-8.
The interaction of mazindol and d-amphetamine with brain monoamines was studied in rats. At each dose used, both compounds markedly counteracted the decrease of brain noradrenaline induced by 6-hydroxydopamine while only at high doses they did significantly reduce the effect of 6-hydroxydopamine on brain dopamine. Unlike d-amphetamine, mazindol significantly counteracted the decrease of brain serotonin induced by fenfluramine. The anorectic effect of mazindol and of d-amphetamine was markedly reduced by an electrolytic lesion at the level of the ventral noradrenergic bundle but not by an electrolytic lesion of the nucleus raphe medianus. An intrastriatal injection of 6-hydroxydopamine significantly reduced the effect of mazindol but not that of d-amphetamine. The results indicate that both compounds may block noradrenaline uptake in the brain while their effect on dopamine uptake is less evident. Ulike d-amphetamine, mazindol appears to inhibit serotonin uptake also. In addition, the integrity of the noradrenergic neurons in the brain appears to be an important condition for these drugs to exert their anorectic effect.
在大鼠中研究了马吲哚和右旋苯丙胺与脑单胺的相互作用。在所使用的每个剂量下，两种化合物均能显著对抗6-羟基多巴胺诱导的脑去甲肾上腺素的减少，而只有在高剂量时它们才会显著降低6-羟基多巴胺对脑多巴胺的作用。与右旋苯丙胺不同，马吲哚能显著对抗芬氟拉明诱导的脑血清素的减少。腹侧去甲肾上腺素能束水平的电解损伤可显著降低马吲哚和右旋苯丙胺的厌食作用，但中缝正中核的电解损伤则无此作用。纹状体内注射6-羟基多巴胺可显著降低马吲哚的作用，但对右旋苯丙胺则无此作用。结果表明，两种化合物均可阻断脑中去甲肾上腺素的摄取，而它们对多巴胺摄取的作用则不太明显。与右旋苯丙胺不同，马吲哚似乎也能抑制血清素的摄取。此外，脑中去甲肾上腺素能神经元的完整性似乎是这些药物发挥其厌食作用的重要条件。
