Pharmacological activity of novel GABA re-uptake inhibitors in mice


γ-aminobutyric acid
γ-hydroxybutyric acid
GABA transporters

How to Cite

Podkowa A, Grzywa A, Lechocka A, Szlonzak A, Kowalczyk P, Kulig K, Filipek B, Sałat K. Pharmacological activity of novel GABA re-uptake inhibitors in mice. mir [Internet]. 30Jun.2014 [cited 1Dec.2021];(102):32-0. Available from:


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 alsoinvestigate 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 alsodemonstrateantidepressant-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 impairments. The obtained results suggest that compounds targeting at GABA transporters may exert analgesic and antidepressant-like properties.