Francesca F, Baggio G
Life Sci. 1985 Apr 8;36(14):1397-405. doi: 10.1016/0024-3205(85)90046-3.
Imidazole (IMI) (from 18.7 to 300 mg/Kg) i.p. injected in adult rats induced shaking, which was antagonized by both morphine (MOR) and haloperidol (HALO) but not by methysergide (MET). I.p. IMI pretreatment inhibited the penile erections (PE) and stretching and yawning (SY) typically elicited by N-n-propylnorapomorphine (NPA), a well-known CNS dopamine (DA) receptor stimulant, injected either i.p. or i.c.v., whereas it enhanced stereotyped behavior (SB). IMI had similar effects on the same parameters considered when injected before lisuride, an ergot derivative also active as a central DA receptor agonist. In this case not only SB but also and above all aggressiveness were markedly potentiated, both the signs appearing at doses of lisuride which were "per se" ineffective. Aggressiveness, like SB, was not sex linked and was antagonized by HALO and MOR, but not by MET. IMI alone potentiated the fighting induced by electrical shock, an effect which was abolished by HALO pretreatment. Considering the results obtained as a whole it is submitted that IMI antagonizes PE and SY through a selective blockade of a class of DA receptors, presumably DA presynaptic autoinhibitors, thus potentiating SB and aggressiveness, which involve stimulation of DA postsynaptic receptors.
腹腔注射咪唑(IMI)(剂量为18.7至300毫克/千克)可诱发成年大鼠颤抖,吗啡(MOR)和氟哌啶醇(HALO)均可拮抗这种颤抖,但甲基麦角新碱(MET)则不能。腹腔注射IMI预处理可抑制由N-正丙基去甲阿扑吗啡(NPA,一种著名的中枢神经系统多巴胺(DA)受体兴奋剂)经腹腔或脑室内注射后通常引发的阴茎勃起(PE)以及伸展和打哈欠(SY),然而却增强了刻板行为(SB)。当在麦角酰二乙胺(一种同样作为中枢DA受体激动剂的麦角衍生物)注射前注射IMI时,对相同参数也有类似影响。在这种情况下,不仅SB,而且最重要的是攻击性均明显增强,这两种表现均出现在麦角酰二乙胺“本身”无效的剂量下。攻击性与SB一样,与性别无关,可被HALO和MOR拮抗,但不能被MET拮抗。单独使用IMI可增强电击诱发的打斗,这种效应可被HALO预处理消除。综合考虑所获得的结果,认为IMI通过选择性阻断一类DA受体(可能是DA突触前自身抑制剂)来拮抗PE和SY,从而增强SB和攻击性,而SB和攻击性涉及DA突触后受体的刺激。