Maj J, Rogóz Z, Skuza G
Eur J Pharmacol. 1982 Jul 9;81(2):287-92. doi: 10.1016/0014-2999(82)90446-0.
Fluvoxamine, (E)-5-methoxy-4'-(trifluoromethyl)valerophenone O-2(2-aminoethyl)oxime, a new antidepressant drug inhibiting serotonin (5-HT) uptake, was studied in rats and mice in order to check whether it has any central anti-5-HT activity, as do some tricyclic antidepressants, e.g. amitriptyline and doxepin. Fluvoxamine did not influence either the 5-hydroxytryptophan-induced head twitch response in mice or the tryptamine convulsions in rats. In the hind limb flexor reflex of the spinal rat the stimulation induced by fenfluramine was inhibited, that induced by LSD was not changed. Fluvoxamine also antagonized the hyperthermia (at ambient temperature of 28 degrees C), induced in rats by fenfluramine or p-chloroamphetamine. The hyperthermia caused by m-chlorophenylpiperazine was not inhibited. Fluvoxamine did not antagonize the 5-HT pressor effect in pithed rats. It has no effect on the immobility time in the behavioural despair test in rats. The results indicate that fluvoxamine fails to show anti-5-HT activity.
氟伏沙明,即(E)-5-甲氧基-4'-(三氟甲基)戊酰苯O-2(2-氨基乙基)肟,是一种新型的抑制血清素(5-HT)摄取的抗抑郁药物。为了检验它是否像某些三环类抗抑郁药(如阿米替林和多塞平)那样具有中枢抗5-HT活性,我们在大鼠和小鼠身上对其进行了研究。氟伏沙明既不影响小鼠中5-羟色氨酸诱导的头部抽搐反应,也不影响大鼠中的色胺惊厥。在脊髓大鼠的后肢屈肌反射中,芬氟拉明诱导的刺激受到抑制,而麦角酸二乙胺诱导的刺激则没有变化。氟伏沙明还拮抗了芬氟拉明或对氯苯丙胺在大鼠中(在环境温度为28摄氏度时)诱导的体温过高。间氯苯哌嗪引起的体温过高没有受到抑制。氟伏沙明不能拮抗脊髓麻醉大鼠中的5-HT升压作用。它对大鼠行为绝望试验中的不动时间没有影响。结果表明,氟伏沙明没有显示出抗5-HT活性。