Inhibitory effect of theophylline on recombinant GABAA receptor
Inhibitory effect of theophylline on recombinant GABAA receptor
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DOI：
10.1097/00001756-200103050-00013
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发表时间：
2001-03-05
期刊：
影响因子：
1.7
通讯作者：
Okada, S
中科院分区：
文献类型：
--
作者：
Sugimoto, T;Sugimoto, M;Okada, S
全身毒性引起的惊厥是茶碱的主要且常常致命的副作用。茶碱引起惊厥的原因尚不清楚，但可能与抑制性神经系统的拮抗作用有关。因此，我们使用重组 GABA(A) 受体 (GABA(A)-R) 检测了茶碱对 GABA 诱导电流的影响。茶碱剂量依赖性地抑制GABA诱导的电流：IC50值为1841+/-63μM，Hill系数为1.09+/-0.03。茶碱对 GABA 感应电流的抑制作用是竞争性的且依赖于电压。茶碱对 GABA 诱导电流的抑制可能是茶碱诱导惊厥的主要机制。 NeuroReport 12:489-493 (C) 2001 Lippincott Williams & Wilkins。
Convulsions due to systemic toxicity are a major and frequently fatal side effect of theophylline. The cause of theophylline-induced convulsions is not clear, but antagonism of the inhibitory nervous system may be implicated. so we examined the effects of theophylline on GABA-induced currents using recombinant GABA(A) receptor (GABA(A)-R). Theophylline dose-dependently inhibited GABA-induced currents: the IC50 value was 1841 +/- 63 muM and Hill coefficient 1.09 +/- 0.03. The inhibitory action of theophylline on GABA-induced currents was competitive and voltage dependent. The inhibition of GABA-induced currents by theophylline may be a primary mechanism underlying theophylline-induced convulsions. NeuroReport 12:489-493 (C) 2001 Lippincott Williams & Wilkins.