Ueki S, Fujiwara M, Inoue K, Kataoka Y, Ibii N
Nihon Yakurigaku Zasshi. 1975 Nov;71(8):789-815. doi: 10.1254/fpj.71.789.
The effect of maprotiline (N-methyl-9, 10-ethanoanthracene-9 (10H)-propylamine) on animal behavior was investigated in mice and rats and compared with those of amitriptyline and imipramine. Maprotiline inhibited reserpine hypothermia in mice and tetrabenazine ptosis in rats, while it potentiated the effects of methamphetamine, L-DOPA and apomorphine in mice, in a similar manner to that of amitriptyline and imipramine. Maprotiline was more potent than anitriptyline and imipramine in antagonizing haloperidol-induced catalepsy as well as in suppressing muricide induced by either olfactory bulbectomy or delta-9-tetrahydrocannabinol in rats. Maprotiline potentiated anesthesia induced by thiopental or ether in mice to a lesser degree than did amitriptyline, and failed to counteract the lethal effect of physostigmine or oxotremorine tremor in mice, indicating that this drug has no central anti-cholinergic effect. Maprotiline markedly inhibited hyperemotionality of the rat with either septal lesions or olfactory bulb ablations, suggesting that it does have a tranquilizing effect. Inhibition of conditioned avoidance response of the rat in the shuttle box and reduction of methamphetamine group toxicity with maprotiline were similar to those with amitriptyline. Maprotiline exaggerated pentetrazol convulsion, decreased muscle tone and impaired coordinated motor activity in mice to a much lesser degree than amitriptyline and imipramine. LD50 of maprotiline was approximately twice that of imipramine and three times that of amitriptyline. These results indicate that maprotiline is a new type of antidepressant, has a low toxicity and shares both potent antidepressant and some tranquilizing effect, without possessing central anticholinergic action.
研究了马普替林(N-甲基-9,10-亚乙基蒽-9(10H)-丙胺)对小鼠和大鼠动物行为的影响,并与阿米替林和丙咪嗪进行了比较。马普替林可抑制小鼠的利血平性体温过低以及大鼠的丁苯那嗪性眼睑下垂,同时它增强了小鼠体内甲基苯丙胺、左旋多巴和阿扑吗啡的作用,其方式与阿米替林和丙咪嗪相似。在拮抗氟哌啶醇诱导的僵住症以及抑制大鼠嗅球切除或δ-9-四氢大麻酚诱导的杀鼠行为方面,马普替林比阿米替林和丙咪嗪更有效。马普替林增强硫喷妥钠或乙醚诱导的小鼠麻醉的程度低于阿米替林,并且无法对抗毒扁豆碱或氧化震颤素引起的小鼠震颤的致死效应,这表明该药物没有中枢抗胆碱能作用。马普替林显著抑制有隔区损伤或嗅球切除的大鼠的过度情绪反应,表明它确实具有镇静作用。马普替林对大鼠穿梭箱条件性回避反应的抑制以及对甲基苯丙胺组毒性的降低与阿米替林相似。马普替林使小鼠戊四氮惊厥加剧、肌肉张力降低和协调运动活动受损的程度远低于阿米替林和丙咪嗪。马普替林的半数致死量约为丙咪嗪的两倍和阿米替林的三倍。这些结果表明,马普替林是一种新型抗抑郁药,毒性低,兼具强效抗抑郁和一定的镇静作用,且不具有中枢抗胆碱能作用。