McAllister K H
Sandoz Research Institute Berne Ltd., Switzerland.
Eur J Pharmacol. 1993 Feb 9;231(2):309-12. doi: 10.1016/0014-2999(93)90467-v.
The effects of blockade of the alpha-amino-3-hydroxy-5-methyl-isoxazole-4-proprionate (AMPA) and kainate subtypes of NBQX (2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline) and compared to the effects of N-methyl-D-aspartate (NMDA) receptor blockade with D-CPPene (D-(E)-4-(3-phosphonoprop-2-enyl)-piperazine-2-carboxylic acid), a competitive NMDA antagonist. Both compounds exerted peak blocking activity 30 min after intraperitoneal administration. Using this pretreatment interval, a dose-response relationship for blocking handling-induced, strychnine-potentiated convulsions was generated for each compound. D-CPPene blocked seizures with an ED50 of 0.72 (0.59-0.87) mg/kg and NBQX blocked seizures with an ED50 of 68.0 (36.72-125.94) mg/kg. These results indicate that both NMDA and non-NMDA subtypes of excitatory amino acid receptors are activated in handling-induced, strychnine-potentiated convulsions.
研究了2,3 - 二羟基 - 6 - 硝基 - 7 - 氨磺酰基 - 苯并(F)喹喔啉（NBQX）对α - 氨基 - 3 - 羟基 - 5 - 甲基 - 异恶唑 - 4 - 丙酸（AMPA）和海人藻酸亚型受体的阻断作用，并与竞争性N - 甲基 - D - 天冬氨酸（NMDA）受体拮抗剂D - (E) - 4 - (3 - 膦酰基 - 2 - 烯丙基) - 哌嗪 - 2 - 羧酸（D - CPPene）对NMDA受体的阻断作用进行比较。两种化合物腹腔注射后30分钟均发挥出最大阻断活性。利用这个预处理间隔时间，分别得出了每种化合物对阻断处理诱导的、士的宁增强的惊厥的剂量 - 反应关系。D - CPPene阻断惊厥的半数有效剂量（ED50）为0.72（0.59 - 0.87）mg/kg，NBQX阻断惊厥的ED50为68.0（36.72 - 125.94）mg/kg。这些结果表明，在处理诱导的、士的宁增强的惊厥中，兴奋性氨基酸受体的NMDA和非NMDA亚型均被激活。
