Evaluation of β-amino carboxylic acid derivatives in hippocampal excitatory synaptic transmission

Daniela Rodrigues de Oliveira, Zuner Bortolotto, Joao Fernandes, Cibele Venancio Luchez

Research output: Contribution to journalArticle (Academic Journal)peer-review

Abstract

β-Aminocarboxylic acid derivatives (LINS04 series) were screened with the aim to explore their potential functional role in excitatory synaptic transmission in the central nervous system. We used field recordings in rat hippocampal slices to investigate the effects of the LINS04 series on the synaptic transmission at hippocampal CA1 synapses. We found that LINS04008 and LINS04009 increase the size of the evoked field excitatory postsynaptic potential (EPSP) in a dose dependent manner. The concentration–response curve shows that
the efficacy of LINS04008 is highest in the series (EC50 = 91.32 µM; maximum fEPSP 44.97%). The esters LINS04006 and LINS04005 did not affect the synaptic evoked activity. These data provide the first evidence of synaptic activity enhancement by these compounds and the importance of the acidic group to the activity. This set of data may provide direction for a strategic procedure to restore the glutamate synaptic transmission; however, further studies are needed to establish a more complete picture of how these molecules act on the
glutamate transmission, which are in our mind for the next steps.
Original languageEnglish
Number of pages7
JournalArchiv der Pharmazie
Early online date5 Sep 2017
DOIs
Publication statusE-pub ahead of print - 5 Sep 2017

Keywords

  • β-Amino acids
  • β-Amino esters
  • Excitatory Postsynaptic Potentials
  • Hippocampus
  • Synaptic Transmission

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