1429322-07-5Relevant academic research and scientific papers
Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides
Kowalczyk, Paula,Sa?at, Kinga,H?fner, Georg C.,Mucha, Marta,Rapacz, Anna,Podkowa, Adrian,Filipek, Barbara,Wanner, Klaus T.,Kulig, Katarzyna
, p. 256 - 273 (2014/07/08)
Six series of 2-substituted 4-aminobutanamide derivatives were synthesized and evaluated for their ability to inhibit GABA transport proteins mGAT1-4 stably expressed in HEK-293 cell lines. The pIC50 values determined were in the range 4.23-5.23. Two compounds (15b and 15c) were selected for further in vitro studies. These compounds were also subjected to preliminary behavioral studies to evaluate their anticonvulsant, antidepressant-like, and antinociceptive activities in mice. Their influence on motor coordination was also assessed. We report that, among a spectrum of in vivo activities, both 15b and 15c displayed significant activity against pentylenetetrazole (PTZ)-induced seizures.
