Home General Physiology and Biophysics 2018 General Physiology and Biophysics Vol.37, No.3, p.299–307, 2018

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Quarterly, 80 pp. per issue
Founded: 1982
ISSN  1338-4325 (online)

Published in English

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General Physiology and Biophysics Vol.37, No.3, p.299–307, 2018

Title: SNC80 and naltrindole modulate voltage-dependent sodium, potassium and calcium channels via a putatively delta opioid receptor-independent mechanism
Author: Lucia Moravčíková, Jana Královičová, Ľubica Lacinová

Abstract: SNC80 was designed as a highly selective nonpeptide delta opioid receptor (DOR) agonist.
Antidepressant-like and antinociceptive effects of this compound were demonstrated in animal
models. Naltrindole was synthetized as a highly selective DOR antagonist. Its antitussive and antinociceptive
effects were reported. Observed effects of SNC80 and naltrindole may be accompanied
by changes in neuronal excitability including modulation of voltage-dependent ion channels. We
investigated possible DOR-independent modulation of neuronal sodium, calcium and potassium
currents by both agents. NG108-15 cells lacking expression of DOR protein were used as model of
neuronal cells. Cells were differentiated into neuronal phenotype by exposure to dibutyryl cyclic-
AMP (dbcAMP). Lack of DORs expression in NG108-15 cells and the presence of DOR expression
in brain and neuronal cultures were demonstrated by Western blot analysis. Both SNC80 and
naltrindole exerted low to moderate modulatory effects on voltage-dependent ion currents. SNC80
weakly inhibited sodium current, potentiated calcium current, and did not act on potassium channels.
Naltrindole inhibited sodium current, did not act on calcium current and inhibited potassium
current at a high concentration. Such effects should be taken into account when these compounds
are used for investigation of DOR-mediated signaling pathways.

Keywords: NG108-15 cells, Naltrindole, SNC80, Sodium current, Potassium current, Calcium current, Opioid receptors
Published online: 31-May-2018
Year: 2018, Volume: 37, Issue: 3 Page From: 299, Page To: 307

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