In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator.

@article{Porcu2016InVA,
  title={In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator.},
  author={Alessandra Porcu and Carla Lobina and Daniela Giunta and Maurizio Solinas and Claudia Mugnaini and Maria Paola Castelli},
  journal={European journal of pharmacology},
  year={2016},
  volume={791},
  pages={
          115-123
        }
}
Positive allosteric modulators (PAMs) of the GABAB receptor have emerged as a novel approach to the pharmacological manipulation of the GABAB receptor, enhancing the effects of receptor agonists with few side effects. Here, we identified N-cyclohexyl-4-methoxy-6-(4-(trifluoromethyl)phenyl)pyrimidin-2-amine (SSD114) as a new compound with activity as a GABAB PAM in in vitro and in vivo assays. SSD114 potentiated GABA-stimulated [35S]GTPγS binding to native GABAB receptors, whereas it had no… Expand
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