2010年12月
Remarkable selectivity of the in vivo binding of [3H]Ro15-4513 to α5 subtype of benzodiazepine receptor in the living mouse brain.
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- 巻
- 64
- 号
- 12
- 開始ページ
- 928
- 終了ページ
- 936
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1002/syn.20812
To evaluate the binding characteristics of [(3)H]Ro15-4513 with the central benzodiazepine (BZ) receptor, inhibition experiments of [(3)H]Ro15-1788 and [(3)H]Ro15-4513 were performed both in vitro and in vivo, using two BZ ligands, flunitrazepam (FNP), and ethyl-β-carboline-3-carboxylate (β-CCE). FNP inhibited the binding of [(3)H]Ro15-1788 and [(3)H]Ro15-4513 in a dose-dependent manner in the mouse cerebral cortex, hippocampus, and cerebellum, both in vitro and in vivo. β-CCE also inhibited the binding of [(3)H]Ro15-1788 and [(3)H]Ro15-4513 in all the aforementioned brain regions in vitro. However, in vivo, β-CCE inhibited the binding of [(3)H]Ro15-4513 in the cerebral cortex and cerebellum, but not in the hippocampus, even at an injected dose of up to 1mg/kg. In contrast, more than 50% of the in vivo binding of [(3)H]Ro15-1788 was inhibited by 1 mg/kg of β-CCE in all regions. The time-activity curve of [(3)H]Ro15-4513 in the hippocampus also showed no alteration of the peak uptake between the control group and 0.3 mg/kg of β-CCE coinjected group. These results indicated that the binding characteristics of [(3)H]Ro15-4513 with the BZ receptor differed markedly between the in
- リンク情報
- ID情報
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- DOI : 10.1002/syn.20812
- ISSN : 0887-4476
- Web of Science ID : WOS:000283611600006