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Dernière publication 01/07/2015

Novel Spirohydantoin Derivative as a Potent Multireceptor-Active Antipsychotic a

A series of novel spirohydantoin derivatives with arylpiperazinylbutyl moiety were synthesized and evaluated for serotonin 5-HT1A, 5-HT2A, 5-HT7...

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    [title] => Novel Spirohydantoin Derivative as a Potent Multireceptor-Active Antipsychotic a
    [paragraph] => Novel Spirohydantoin Derivative as a Potent Multireceptor-Active Antipsychotic and Antidepressant Agent
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Authors
Czopek A, Ko?aczkowski M, Bucki A, Byrtus H et al.

 Lab
Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Kraków, Poland
Journal
Bioorg Med Chem.
Abstract
A series of novel spirohydantoin derivatives with arylpiperazinylbutyl moiety were synthesized and evaluated for serotonin 5-HT1A, 5-HT2A, 5-HT7 and dopamine D2 receptors. Based on these data, four compounds were selected for further binding affinity assays on dopamine D1, D3, D4, and 5-HT2C, 5-HT6 as well as adrenergic ?1 and ?2C receptors, which are involved in various CNS diseases such as schizophrenia, anxiety and/or depression. The compound 14, 1-{4-[4-(2-metoxyphe-nyl)piperazin-1-yl]butyl}-3,4-dihydro-2H,2H,5H-spiro[imidazolidine-4,1-naphthalene]-2,5-dione, with the most promising functional profile, mixed 5-HT2A/D2 antagonist and 5-HT1A partial agonist, was selected. In the mouse d-amphetamine-induced locomotor hyperactivity model, compound 14 produced antipsychotic-like activity, which is devoid of cataleptogenic effects and in the forced swim test in mice, it showed a significant antidepressant-like effect unlike the reference drug aripiprazole.
BIOSEB Instruments Used
Forced Swimming Test: New FST DUAL SENSOR (BIO-FST-DSM)
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Le nouveau Test de Nage Forcée Bioseb DUAL SENSOR à été développé selon une double approche:
En combinant une double acquisition, vibrations et trace vidéo,
 l'algorithme TYC (Train-Your-Computer) compare les deux sources capteur pour déterminer en temps réel le comportement de l'animal, rendant les résultats complètement indépendants de l'opérateur.

Le gestionnaire d'expériences, le module d'analyse, les possibilités de relecture et l'algorithme TYC sont parmi les fonctionnalités qui font du FST DUAL SENSOR un instrument très innovant et facile d'utilisation pour les études sur rats et souris (jusqu'à 4 animaux à la fois) pour automatiser le test de Porsolt, ou test de désespoir comportemental.

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