Effect of 5-{3-(4-(4-fluorophenyl)-1-piperazinyl)-propoxy}indan(BP-528) on benzodiazepine receptor bindings and .GAMMA.-aminobutyric acid release.
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概要
- 論文の詳細を見る
The action of a new type of anti-anxiety compound, 5-{3-[4-(4-fluorophenyl)-1-piperazinyl]-propoxy}indan (BP-528), was tested on benzodiazepine receptor bindings and on [<SUP>3</SUP>H]-GABA release. BP-528 did not alter [<SUP>3</SUP>H]-diazepam binding to rat cerebral cortical and hippocampal membranes either in the presence or absence of GABA; and the binding of [<SUP>3</SUP>H]-propyl-β-carboline-3-carboxylate at low concentration (0.04 nM), which labels only the type I benzodiazepine receptor, was not changed by BP-528. BP-528 did not interact with the GABA-benzodiazepine receptor complex, which is related to the anti-anxiety activity of benzodiazepines. This compound affected neither GABA binding nor GABA uptake. Ten micromolar BP-528 depressed high K<SUP>+</SUP>-induced [<SUP>3</SUP>H]-GABA release from preloaded rat hippocampal slices. However, the same concentration of BP-528 also inhibited high K<SUP>+</SUP>-induced calcium uptake by rat cerebral cortical synaptosomes.
- 公益社団法人 日本薬理学会の論文
著者
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Baba Akemichi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Osaka University
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Iwata Heitaroh
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Osaka University
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Ohta Akira
Department Of Applied Chemistry Faculty Of Engineering Kogakuin University
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