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

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

doi:10.1002/ardp.201700179

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 journal › Article (Academic Journal) › peer-review

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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 language	English
Number of pages	7
Journal	Archiv der Pharmazie
Early online date	5 Sept 2017
DOIs	https://doi.org/10.1002/ardp.201700179
Publication status	E-pub ahead of print - 5 Sept 2017

Keywords

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

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@article{6650ed1a378e4d4eb37ff31bbd30799f,

title = "Evaluation of β-amino carboxylic acid derivatives in hippocampal excitatory synaptic transmission",

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 thatthe 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 theglutamate transmission, which are in our mind for the next steps. ",

keywords = "β-Amino acids , β-Amino esters, Excitatory Postsynaptic Potentials, Hippocampus, Synaptic Transmission",

author = "{Rodrigues de Oliveira}, Daniela and Zuner Bortolotto and Joao Fernandes and {Venancio Luchez}, Cibele",

year = "2017",

month = sep,

day = "5",

doi = "10.1002/ardp.201700179",

language = "English",

journal = "Archiv der Pharmazie",

issn = "0365-6233",

publisher = "Wiley-VCH Verlag",

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TY - JOUR

T1 - Evaluation of β-amino carboxylic acid derivatives in hippocampal excitatory synaptic transmission

AU - Rodrigues de Oliveira, Daniela

AU - Bortolotto, Zuner

AU - Fernandes, Joao

AU - Venancio Luchez, Cibele

PY - 2017/9/5

Y1 - 2017/9/5

N2 - 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 thatthe 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 theglutamate transmission, which are in our mind for the next steps.

AB - 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 thatthe 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 theglutamate transmission, which are in our mind for the next steps.

KW - β-Amino acids

KW - β-Amino esters

KW - Excitatory Postsynaptic Potentials

KW - Hippocampus

KW - Synaptic Transmission

U2 - 10.1002/ardp.201700179

DO - 10.1002/ardp.201700179

M3 - Article (Academic Journal)

C2 - 28872703

SN - 0365-6233

JO - Archiv der Pharmazie

JF - Archiv der Pharmazie

ER -

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

Abstract

Keywords

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