Ueki S, Yamamoto T, Shimazoe T, Shibata S, Tani Y, Machida K, Hojo M, Yoshida Y, Tatsumi H
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Nihon Yakurigaku Zasshi. 1988 Jun;91(6):359-69. doi: 10.1254/fpj.91.359.
The effects of a new tricyclic antidepressant quinupramine (5-(3-quinuclidinyl)-10,11-dihydro-5H-dibenz [b, f] azepine) on various animal behaviors were examined in mice and rats and compared with those of imipramine, amitriptyline and maprotiline. Quinupramine antagonized haloperidol-induced catalepsy and tetrabenazine-induced ptosis and potentiated methamphetamine- and apomorphine-induced stereotyped behavior. These effects were almost the same as or even more potent than those of imipramine and amitriptyline. Quinupramine decreased locomotor activity in mice, but potentiated methamphetamine-induced hyperactivity to a greater degree than imipramine and amitriptyline. On the other hand, quinupramine inhibited muricide in accumbens-lesioned rats, but did not prominently inhibit muricide in olfactory-bulbectomized and raphe-lesioned rats. Quinupramine decreased the duration of immobility in low doses without affecting locomotor activity, and this effect was almost the same as that of imipramine and amitriptyline and more potent than that of maprotiline. Quinupramine antagonized physostigmine lethality and oxotremorine-induced tremor, suggesting that quinupramine has a central anticholinergic action. Quinupramine, like imipramine and amitriptyline, has no effect on conditioned avoidance behavior. In conclusion, quinupramine generally has the same behavioral profile as typical tricyclic antidepressants, but it has somewhat different effects from imipramine and amitriptyline since quinupramine has a potent central anticholinergic and a weak antimuricide effect.
研究了一种新型三环抗抑郁药喹诺普明(5-(3-喹核啶基)-10,11-二氢-5H-二苯并[b,f]氮杂卓)对小鼠和大鼠各种动物行为的影响,并与丙咪嗪、阿米替林和马普替林进行了比较。喹诺普明拮抗氟哌啶醇诱导的僵住症和丁苯那嗪诱导的眼睑下垂,并增强甲基苯丙胺和阿扑吗啡诱导的刻板行为。这些作用与丙咪嗪和阿米替林的作用几乎相同,甚至更强。喹诺普明降低了小鼠的自发活动,但比丙咪嗪和阿米替林更能增强甲基苯丙胺诱导的活动亢进。另一方面,喹诺普明抑制伏隔核损伤大鼠的杀鼠行为,但对嗅球切除和中缝损伤大鼠的杀鼠行为没有明显抑制作用。喹诺普明在低剂量时缩短了不动时间,而不影响自发活动,这种作用与丙咪嗪和阿米替林几乎相同,且比马普替林更强。喹诺普明拮抗毒扁豆碱致死作用和氧化震颤素诱导的震颤,提示喹诺普明具有中枢抗胆碱能作用。喹诺普明与丙咪嗪和阿米替林一样,对条件回避行为没有影响。总之,喹诺普明的一般行为特征与典型的三环抗抑郁药相同,但它与丙咪嗪和阿米替林有一些不同的作用,因为喹诺普明具有较强的中枢抗胆碱能作用和较弱的抗杀鼠行为作用。