Publications

Dernière publication 10/07/2013

Evaluation of anxiolytic-like- anticonvulsant- antidepressant-like and antinocic

Purpose The inhibition of plasma membrane GABA transporters (GATs) is responsible for anxiolytic-like, anticonvulsant, antinociceptive and...

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    [title] => Evaluation of anxiolytic-like- anticonvulsant- antidepressant-like and antinocic
    [paragraph] => Evaluation of anxiolytic-like, anticonvulsant, antidepressant-like and antinociceptive properties of new 2-substituted 4-hydroxybutanamides with affinity for GABA transporters in mice
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Authors
K. Sałata, K. Kuligb, J. Gajdab, K. Więckowskib, B. Filipeka et al.

 Lab
Jagiellonian University, Medical College, Cracow, Poland
Journal
Pharmacology Biochemistry and Behavior
Abstract
Purpose
The inhibition of plasma membrane GABA transporters (GATs) is responsible for anxiolytic-like, anticonvulsant, antinociceptive and antidepressant-like effects in mice. It also influences animals' motor coordination and their sensitivity to ethanol. The aim of this study was to assess the pharmacological activity of two novel 2-substituted 4-hydroxybutanamides (BM 130 and BM 131) in some screening models. An attempt has been made to establish the relationship between the inhibition of GAT subtype and the observed in vivo activity.
Methods
The affinity for GAT subtypes was evaluated by means of [3H]GABA uptake assay. It indicated that BM 130 inhibited GAT1 and GAT2, whereas BM 131 inhibited GAT1 and GAT3. In mice anxiolytic-like, antidepressant-like, anticonvulsant and antinociceptive properties of the test compounds were assessed. Their influence on motor coordination, locomotor activity and the ability to potentiate effects of subnarcotic doses of ethanol was also tested.
Results
Both compounds administered intraperitoneally exerted a significant anxiolytic-like effect in the four plate test with ED50 values 3.4 and 7.9 mg/kg, respectively. At 30 mg/kg they reduced duration of immobility in the forced swim test for 33% and 19%, respectively. They had no effect on electroconvulsive threshold or pain reactivity in the hot plate assay but they were antinociceptive in the acetic acid-induced writhing test (ED50 values were 12.7 and 18.6 mg/kg, respectively) and in both phases of the formalin test (ED50 values in the first phase were 10.2 and 2.1 mg/kg for BM 130 and BM 131, respectively). No motor adverse effects were observed in mice pretreated with the test compounds in the rotarod or chimney tests but BM 131 caused a transient but statistically significant decrease of animals' locomotor activity.
Conclusions
In mice BM 130 and BM 131 have anxiolytic-like, antidepressant-like and antinociceptive properties which can be attributed to their affinity for not only mGAT1 but also mGAT2–4.
BIOSEB Instruments Used
Forced Swimming Test: New FST DUAL SENSOR (BIO-FST-DSM)
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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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