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Kir3 channel signaling complexes: focus on opioid receptor signaling

Opioids are among the most effective drugs to treat severe pain. They produce their analgesic actions by specifically activating opioid receptors located along the pain perception pathway where they inhibit the flow of nociceptive information. This inhibition is partly accomplished by activation of...

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Detalles Bibliográficos
Autores principales: Nagi, Karim, Pineyro, Graciela
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4085882/
https://www.ncbi.nlm.nih.gov/pubmed/25071446
http://dx.doi.org/10.3389/fncel.2014.00186
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author Nagi, Karim
Pineyro, Graciela
author_facet Nagi, Karim
Pineyro, Graciela
author_sort Nagi, Karim
collection PubMed
description Opioids are among the most effective drugs to treat severe pain. They produce their analgesic actions by specifically activating opioid receptors located along the pain perception pathway where they inhibit the flow of nociceptive information. This inhibition is partly accomplished by activation of hyperpolarizing G protein-coupled inwardly-rectifying potassium (GIRK or Kir3) channels. Kir3 channels control cellular excitability in the central nervous system and in the heart and, because of their ubiquitous distribution, they mediate the effects of a large range of hormones and neurotransmitters which, upon activation of corresponding G protein-coupled receptors (GPCRs) lead to channel opening. Here we analyze GPCR signaling via these effectors in reference to precoupling and collision models. Existing knowledge on signaling bias is discussed in relation to these models as a means of developing strategies to produce novel opioid analgesics with an improved side effects profile.
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spelling pubmed-40858822014-07-28 Kir3 channel signaling complexes: focus on opioid receptor signaling Nagi, Karim Pineyro, Graciela Front Cell Neurosci Neuroscience Opioids are among the most effective drugs to treat severe pain. They produce their analgesic actions by specifically activating opioid receptors located along the pain perception pathway where they inhibit the flow of nociceptive information. This inhibition is partly accomplished by activation of hyperpolarizing G protein-coupled inwardly-rectifying potassium (GIRK or Kir3) channels. Kir3 channels control cellular excitability in the central nervous system and in the heart and, because of their ubiquitous distribution, they mediate the effects of a large range of hormones and neurotransmitters which, upon activation of corresponding G protein-coupled receptors (GPCRs) lead to channel opening. Here we analyze GPCR signaling via these effectors in reference to precoupling and collision models. Existing knowledge on signaling bias is discussed in relation to these models as a means of developing strategies to produce novel opioid analgesics with an improved side effects profile. Frontiers Media S.A. 2014-07-08 /pmc/articles/PMC4085882/ /pubmed/25071446 http://dx.doi.org/10.3389/fncel.2014.00186 Text en Copyright © 2014 Nagi and Pineyro. http://creativecommons.org/licenses/by/3.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Neuroscience
Nagi, Karim
Pineyro, Graciela
Kir3 channel signaling complexes: focus on opioid receptor signaling
title Kir3 channel signaling complexes: focus on opioid receptor signaling
title_full Kir3 channel signaling complexes: focus on opioid receptor signaling
title_fullStr Kir3 channel signaling complexes: focus on opioid receptor signaling
title_full_unstemmed Kir3 channel signaling complexes: focus on opioid receptor signaling
title_short Kir3 channel signaling complexes: focus on opioid receptor signaling
title_sort kir3 channel signaling complexes: focus on opioid receptor signaling
topic Neuroscience
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4085882/
https://www.ncbi.nlm.nih.gov/pubmed/25071446
http://dx.doi.org/10.3389/fncel.2014.00186
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