Turski W, Turski L, Czuczwar S J, Kleinrok Z
Pharmacol Biochem Behav. 1981 Oct;15(4):545-9. doi: 10.1016/0091-3057(81)90205-7.
(RS)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) was microinjected into the lateral brain ventricle of conscious rats in order to evaluate its pharmacological effects. Microinjection (5 microliter) were made unilaterally and the effects of AMPA were assessed for 6 hr. AMPA produced generalized myoclonic seizures, short lasting hypoactivity followed by hyperactivity and hyperthermia when low doses were injected (0.25-1.0 microgram). When AMPA was injected at higher doses (1.5-5.0 microgram) it produced generalized myoclonic seizures, a hypoactive phase and hypothermia rapidly followed by hyperthermia. As the seizure activity and hypoactive phase receded, AMPA at doses of less than 2.5 microgram produced hyperactivity and wet dog shakes in a dose-related manner. After receiving AMPA at doses of 2.5 and 5.0 microgram, rats developed transient catalepsy. High quantities (5.0 microgram) evoked a spectrum of generalized convulsive seizures lasting for 2-3 hr (1 seizure every 15 min). Biochemical assays showed that AMPA had complex effects on brain aminergic systems. AMPA decreased brain NA while brain DA concentration was slightly increased in a dose dependent manner. Moreover, AMPA increased brain 5-HT and 5-HIAA concentration in a dose- and time-related manner.
将（RS）-α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）微量注射到清醒大鼠的侧脑室，以评估其药理作用。进行单侧微量注射（5微升），并评估AMPA 6小时的作用。注射低剂量（0.25 - 1.0微克）的AMPA时，会引发全身性肌阵挛性癫痫发作，短暂的活动减少随后是活动亢进和体温过高。当注射较高剂量（1.5 - 5.0微克）的AMPA时，会引发全身性肌阵挛性癫痫发作、一个活动减退期和体温过低，随后迅速出现体温过高。随着癫痫活动和活动减退期消退，剂量小于2.5微克的AMPA会以剂量相关的方式产生活动亢进和湿狗样抖动。接受2.5微克和5.0微克剂量的AMPA后，大鼠会出现短暂的僵住症。高剂量（5.0微克）会引发一系列全身性惊厥性癫痫发作，持续2 - 3小时（每15分钟发作一次）。生化分析表明，AMPA对脑胺能系统有复杂的影响。AMPA会降低脑内去甲肾上腺素（NA）水平，而脑内多巴胺（DA）浓度会以剂量依赖的方式略有增加。此外，AMPA会以剂量和时间相关的方式增加脑内5-羟色胺（5-HT）和5-羟吲哚乙酸（5-HIAA）的浓度。
