Department of Developmental Epileptology, Institute of Physiology AS CR, Prague, Czech Republic.
Physiol Res. 2013;62(Suppl 1):S109-14. doi: 10.33549/physiolres.932599.
Antagonists of GABA(B) receptors are expected to have proconvulsant action also in developing brain. Two antagonists (CGP55845 and CGP46381) were tested in a model of cortical epileptic afterdischarges (ADs) in 12-, 18- and 25-day-old rat pups with implanted electrodes. CGP55845 was dissolved in dimethylsulfoxide and the results demonstrated marked proconvulsant action of this solvent which masked possible action of the antagonist. Water soluble antagonist CGP46381 led to marked potentiation of ADs in 12-day-old animals, its action decreased with age, it was negligible in 25-day-old rats. Our results demonstrated important inhibitory role of GABA(B) receptors at very early stages of maturation.
GABA(B) 受体拮抗剂预计也会对发育中的大脑产生致惊厥作用。两种拮抗剂（CGP55845 和 CGP46381）在植入电极的 12、18 和 25 天大的幼鼠皮质癫痫后放电（AD）模型中进行了测试。CGP55845 溶解在二甲基亚砜中，结果表明该溶剂具有明显的致惊厥作用，掩盖了拮抗剂的可能作用。水溶性拮抗剂 CGP46381 导致 12 天大的动物 AD 明显增强，其作用随年龄而降低，在 25 天大的大鼠中则可忽略不计。我们的结果表明，GABA(B) 受体在成熟的早期阶段发挥着重要的抑制作用。
