Neuman R S, White S R
Eur J Pharmacol. 1982 Jun 16;81(1):49-56. doi: 10.1016/0014-2999(82)90600-8.
The actions of iontophoretically applied quipazine (QPZ) and 6-chloro-2-[1-piperazinyl]-pyrazine (CPP) were compared with those of serotonin (5-HT) on rat spinal motoneurones. QPZ and CPP qualitatively resembled 5-HT in that both facilitated single unit activity evoked by glutamate. Like 5-HT, the facilitation they produced could be antagonized by metergoline or methysergide. These observations are compatible with the suggestion that the actions of QPZ and CPP are mediated by 5-HT receptors. In rats pretreated with the neurotoxin 5,7-dihydroxytryptamine (5,7-DHT), QPZ and CPP remained effective in facilitating the glutamate evoked activity, whereas p-chloroamphetamine (PCA), a known releaser of 5-HT, was without effect. In contrast, PCA produced a long lasting facilitation in untreated rats. These data, taken together, suggest that QPZ and CPP are direct agonists at 5-HT receptors, but do not preclude the possibility that they might also act indirectly.
将离子电渗法应用的喹哌嗪(QPZ)和6-氯-2-[1-哌嗪基]-吡嗪(CPP)与5-羟色胺(5-HT)对大鼠脊髓运动神经元的作用进行了比较。QPZ和CPP在性质上类似于5-HT,因为二者均能促进由谷氨酸诱发的单单位活动。与5-HT一样,它们所产生的促进作用可被麦角新碱或甲基麦角酰胺拮抗。这些观察结果与QPZ和CPP的作用是由5-HT受体介导的这一观点相符。在用神经毒素5,7-二羟基色胺(5,7-DHT)预处理的大鼠中,QPZ和CPP在促进谷氨酸诱发的活动方面仍然有效,而对氯苯丙胺(PCA),一种已知的5-HT释放剂,则没有效果。相比之下,PCA在未处理的大鼠中产生了持久的促进作用。综合这些数据表明,QPZ和CPP是5-HT受体的直接激动剂,但并不排除它们也可能间接起作用的可能性。