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标题：Influence of Plasma Dialysate from Normal and Renal Dysfunction Rats on the Electroencephalogram and γ-Aminobutyric AcidA Receptor Complex Modulation of Thiopental
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作者：Kalpana SRIVASTAVA ; Tomomi HATANAKA ; Kazunori KATAYAMA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1999
卷号：22
期号：3
页码：288-294
DOI：10.1248/bpb.22.288
出版社：The Pharmaceutical Society of Japan
摘要：We have previously reported that brain sensitivity to thiopental with respect to electroencephalogram (EEG) is enhanced in uranyl acetate pretreated renal dysfunction rats. The results were attributed to pharmacodynamic factors. In this study, in vivo EEG and in vitro binding studies for γ-aminobutyric acid (GABA)-benzodiazepine receptor complex were performed to investigate the mechanism of the enhanced effect of thiopenta. The receptor binding properties in the brain membrane from normal and renal dysfunction rats were examined using [³H]tert-buthylbicycloorthobenzoate (TBOB), [³H]flunitrazepam and [³H]muscimol. The effect of plasma dialysate from normal (ND) and renal dysfunction rats (RDD) on the thiopental induced EEG and receptor binding were also examined to confirm the role of endogenous compounds. The intrinsic receptor binding characteristics of various sites and their allosteric interaction with thiopental was similar in membrane preparations from normal and renal dysfunction rats. However, RDD, when compared to ND, enhanced the EEG induced by thiopental. At the receptor level, RDD significantly enhanced the thiopental induced inhibition of TBOB. No difference was found between the influence of ND and RDD on the interaction between thiopental and flunitrazepam or muscimol binding. These results showed that the thiopental induced allosteric inhibition of TBOB binding was potentiated by some endogenous compounds in RDD and suggests that this action might be the mechanism, at least in part, for the increased sensitivity of thiopental in renal dysfunction rats.
关键词：thiopental;renal dysfunction;plasma dialysate;γ-aminobutyric acidA (GABAA) receptor;tert-butylbicycloorthobenzoate (TBOB)