Effect of 5-{3-[4-(4-Fluorophenyl)-1-Piperazinyl]-Propoxy}indan (BP-528) on Benzodiazepine Receptor Bindings and γ-Aminobutyric Acid Release

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 [3H]-GABA release. BP-528 did not alter [3H]-diazepam binding to rat cerebral cortical and hippocampal membranes either in the pres...

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Bibliographic Details
Published in:Japanese journal of pharmacology 1987, Vol.44 (4), p.493-497
Main Authors: OHTA, Akira, BABA, Akemichi, IWATA, Heitaroh
Format: Article
Language:English
Subjects:
Biological and medical sciences
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Psycholeptics: tranquillizer, neuroleptic
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
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Summary: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 [3H]-GABA release. BP-528 did not alter [3H]-diazepam binding to rat cerebral cortical and hippocampal membranes either in the presence or absence of GABA; and the binding of [3H]-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 antianxiety activity of benzodiazepines. This compound affected neither GABA binding nor GABA uptake. Ten micromolar BP-528 depressed high K+-induced [3H]-GABA release from preloaded rat hippocampal slices. However, the same concentration of BP-528 also inhibited high K+-induced calcium uptake by rat cerebral cortical synaptosomes.
ISSN:0021-5198
1347-3506
DOI:10.1016/S0021-5198(19)43459-8