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XB-ART-9454
Neuroreport 2001 Mar 05;123:489-93. doi: 10.1097/00001756-200103050-00013.
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Inhibitory effect of theophylline on recombinant GABA(A) receptor.

Sugimoto T , Sugimoto M , Uchida I , Mashimo T , Okada S .


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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 microM 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.

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