Depression - page 3 Scientific Publications

Latest publication 07/01/2015

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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The new Forced Swimming Test system from Bioseb uses a dual approach:
Combining a double input from vibrations and video,
 the TYC (Train-Your-Computer) algorithm compares both inputs to determine the animal's behavior in real time, making results completely operator-independent.

Experiment manager, analysis module, replay possibilities and the TYC algorithm are some of the features that make FST DUAL SENSOR a very innovative and easy to use instrument for both mice or rats studies (up to 4 animals can be tested at a time), based on the famous Porsolt Test, or "behavioral despair" test

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