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Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System

Uliginosin B (ULI) is a natural acylphloroglucinol that has been proposed as a new molecular scaffold for developing analgesic and antidepressant drugs. Its effects seem to be due to its ability to increase monoamines in the synaptic cleft by inhibiting their neuronal uptake without binding to their...

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Autores principales: Stolz, Eveline Dischkaln, da Costa, Paola Fontoura, Medeiros, Liciane Fernandes, Souza, Andressa, Battastini, Ana Maria Oliveira, von Poser, Gilsane Lino, Bonan, Carla, Torres, Iraci L. S., Rates, Stela Maris Kuze
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4819114/
https://www.ncbi.nlm.nih.gov/pubmed/27087824
http://dx.doi.org/10.1155/2016/5890590
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author Stolz, Eveline Dischkaln
da Costa, Paola Fontoura
Medeiros, Liciane Fernandes
Souza, Andressa
Battastini, Ana Maria Oliveira
von Poser, Gilsane Lino
Bonan, Carla
Torres, Iraci L. S.
Rates, Stela Maris Kuze
author_facet Stolz, Eveline Dischkaln
da Costa, Paola Fontoura
Medeiros, Liciane Fernandes
Souza, Andressa
Battastini, Ana Maria Oliveira
von Poser, Gilsane Lino
Bonan, Carla
Torres, Iraci L. S.
Rates, Stela Maris Kuze
author_sort Stolz, Eveline Dischkaln
collection PubMed
description Uliginosin B (ULI) is a natural acylphloroglucinol that has been proposed as a new molecular scaffold for developing analgesic and antidepressant drugs. Its effects seem to be due to its ability to increase monoamines in the synaptic cleft by inhibiting their neuronal uptake without binding to their respective transporters, but its exact mode of action is still unknown. Considering the importance of the purinergic system to pain transmission and its modulation by monoamines availability, the aim of this study was to investigate the involvement of adenosinergic signaling in antinociceptive effect of uliginosin B. The selective adenosine A(1) receptor antagonist DPCPX and the selective A(2A) antagonist ZM 241385 prevented the effect of ULI in the hot-plate test in mice. Pretreatment with inhibitors of adenosine reuptake (dipyridamole) or adenosine deaminase (EHNA) did not affect the ULI effect. On the other hand, its effect was completely prevented by an inhibitor of ecto-5′-nucleotidase (AMPCP). This finding was confirmed ex vivo, whereby ULI treatment increased AMP and ATP hydrolysis in spinal cord and cerebral cortex synaptosomes, respectively. Altogether, these data indicate that activation of A(1) and A(2A) receptors and the modulation of ecto-5′-nucleotidase activity contribute to the antinociceptive effect of ULI.
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spelling pubmed-48191142016-04-17 Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System Stolz, Eveline Dischkaln da Costa, Paola Fontoura Medeiros, Liciane Fernandes Souza, Andressa Battastini, Ana Maria Oliveira von Poser, Gilsane Lino Bonan, Carla Torres, Iraci L. S. Rates, Stela Maris Kuze Evid Based Complement Alternat Med Research Article Uliginosin B (ULI) is a natural acylphloroglucinol that has been proposed as a new molecular scaffold for developing analgesic and antidepressant drugs. Its effects seem to be due to its ability to increase monoamines in the synaptic cleft by inhibiting their neuronal uptake without binding to their respective transporters, but its exact mode of action is still unknown. Considering the importance of the purinergic system to pain transmission and its modulation by monoamines availability, the aim of this study was to investigate the involvement of adenosinergic signaling in antinociceptive effect of uliginosin B. The selective adenosine A(1) receptor antagonist DPCPX and the selective A(2A) antagonist ZM 241385 prevented the effect of ULI in the hot-plate test in mice. Pretreatment with inhibitors of adenosine reuptake (dipyridamole) or adenosine deaminase (EHNA) did not affect the ULI effect. On the other hand, its effect was completely prevented by an inhibitor of ecto-5′-nucleotidase (AMPCP). This finding was confirmed ex vivo, whereby ULI treatment increased AMP and ATP hydrolysis in spinal cord and cerebral cortex synaptosomes, respectively. Altogether, these data indicate that activation of A(1) and A(2A) receptors and the modulation of ecto-5′-nucleotidase activity contribute to the antinociceptive effect of ULI. Hindawi Publishing Corporation 2016 2016-03-21 /pmc/articles/PMC4819114/ /pubmed/27087824 http://dx.doi.org/10.1155/2016/5890590 Text en Copyright © 2016 Eveline Dischkaln Stolz et al. https://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Stolz, Eveline Dischkaln
da Costa, Paola Fontoura
Medeiros, Liciane Fernandes
Souza, Andressa
Battastini, Ana Maria Oliveira
von Poser, Gilsane Lino
Bonan, Carla
Torres, Iraci L. S.
Rates, Stela Maris Kuze
Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System
title Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System
title_full Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System
title_fullStr Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System
title_full_unstemmed Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System
title_short Uliginosin B, a Possible New Analgesic Drug, Acts by Modulating the Adenosinergic System
title_sort uliginosin b, a possible new analgesic drug, acts by modulating the adenosinergic system
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4819114/
https://www.ncbi.nlm.nih.gov/pubmed/27087824
http://dx.doi.org/10.1155/2016/5890590
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