Janusz W, Kleinrok Z
Department of Pharmacology, Medical School, Lublin, Poland.
Neurosci Res. 1989 Nov;7(2):144-53. doi: 10.1016/0168-0102(89)90054-0.
Modification of central serotonergic transmission resulted in alterations of pilocarpine convulsive activity in male Wistar rats. Seizure activity was increased after pizotifen injection and the latency period to onset of convulsions was shortened in animals pretreated with mianserine and quipazine. Stimulation of 5-HT1A receptors with 8-hydroxy-di-N,N-propylaminotetralin (8-OH-DPAT) and blockade of 5-HT1B receptors with cyanopindolol resulted in seizure protection. Intracerebroventricular injections of 5,6-dihydroxytryptamine (5,6-DHT) did not change the protective effect of cyanopindolol. Other agents specifically affecting serotonergic receptors, the agonists 1-(3-chlorophenyl)piperazine (mCPP) and 5-methoxytryptamine (5-MT) and the antagonists spiperone, metergoline, methysergide, cyproheptadine and metoclopramide, did not influence pilocarpine-induced seizures. In conclusion, the present study suggests that the inhibition of pilocarpine-induced seizures may be mediated by stimulation of 5-HT1A and by blockade of 5-HT1B receptors, located probably on the cholinergic terminals.
中枢5-羟色胺能传递的改变导致雄性Wistar大鼠毛果芸香碱惊厥活性的改变。注射匹莫齐特后癫痫活动增强，而用米安色林和喹哌嗪预处理的动物惊厥发作的潜伏期缩短。用8-羟基-二-N，N-丙基氨基四氢萘（8-OH-DPAT）刺激5-HT1A受体并用氰吲哚洛尔阻断5-HT1B受体可起到癫痫保护作用。脑室内注射5,6-二羟基色胺（5,6-DHT）不会改变氰吲哚洛尔的保护作用。其他特异性影响5-羟色胺能受体的药物，激动剂1-（3-氯苯基）哌嗪（mCPP）和5-甲氧基色胺（5-MT）以及拮抗剂螺哌隆、麦角苄酯、甲基麦角新碱、赛庚啶和甲氧氯普胺，均不影响毛果芸香碱诱发的癫痫发作。总之，本研究表明，毛果芸香碱诱发癫痫发作的抑制作用可能是通过刺激5-HT1A以及阻断可能位于胆碱能终末的5-HT1B受体介导的。
