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PHARMACOLOGICAL ACTIVITY OF NOVEL GABA RE-UPTAKE INHIBITORS IN MICE

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PODKOWA A., GRZYWA A., LECHOCKA A., SZLONZAK A., KOWALCZYK P., KULIG K., FILIPEK B., SAŁAT K.

Medicina Internacia Revuo

2014

vol. 26

issue 102

32- 41

Γ-aminobutyric acid (GABA) is a widely distributed neurotransmitter in the mammalian central nerv-ous system. The GABAergic neurotransmission is involved in numerous processes, including neuronal excitability and mood disorders. GABA is removed from the synaptic cleft by specific proteins called plasma membrane GABA transporters. In the present work we focus on antinociceptive and antidepres-sant-like properties of four new GABA re-uptake inhibitors. These compounds are N-benzylamide derivatives of GABA. We also investigate their impact on animal’ locomotor activity and motor coordina-tion. All the examined compounds present analgesic activity in the hot plate test. Most of them also demonstrate antidepressant-like properties in the forced swim test in mice. Similarly to tiagabine, the test compounds significantly affect locomotor activity and some of them cause motor coordination impair-ments. The obtained results suggest that compounds targeting at GABA transporters may exert analgesic and antidepressant-like properties.

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1 Medicina Internacia Revuo

1 2014

1 FILIPEK B.

1 GRZYWA A.

1 KOWALCZYK P.

1 KULIG K.

1 LECHOCKA A.

1 PODKOWA A.

1 SAŁAT K.

1 SZLONZAK A.

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PHARMACOLOGICAL ACTIVITY OF NOVEL GABA RE-UPTAKE INHIBITORS IN MICE