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Efficacy of isothiocyanate-based compounds on different forms of persistent pain
PURPOSE: Current pharmacotherapy for persistent pain related to neuropathy or articular diseases is unsatisfactory, due to the large number of unresponsive patients and side effects. Isothiocyanates (ITCs) are a class of natural or synthetic compounds characterized by the general formula R–NCS. ITCs...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6250104/ https://www.ncbi.nlm.nih.gov/pubmed/30510445 http://dx.doi.org/10.2147/JPR.S161882 |
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author | Lucarini, Elena Micheli, Laura Martelli, Alma Testai, Lara Calderone, Vincenzo Ghelardini, Carla Di Cesare Mannelli, Lorenzo |
author_facet | Lucarini, Elena Micheli, Laura Martelli, Alma Testai, Lara Calderone, Vincenzo Ghelardini, Carla Di Cesare Mannelli, Lorenzo |
author_sort | Lucarini, Elena |
collection | PubMed |
description | PURPOSE: Current pharmacotherapy for persistent pain related to neuropathy or articular diseases is unsatisfactory, due to the large number of unresponsive patients and side effects. Isothiocyanates (ITCs) are a class of natural or synthetic compounds characterized by the general formula R–NCS. ITCs show antihyperalgesic effects in models of central and peripheral nervous tissue injury and anti-inflammatory properties. The pharmacodynamics are strictly related to the release of the gasotransmitter hydrogen sulfide (H(2)S) from their moiety. In particular, phenyl ITC (PITC) and 3-carboxyphenyl ITC (3C-PITC) exhibit interesting slow H(2)S-release properties suitable for treating painful pathology. The aim of the present work was to evaluate the efficacy of PITC and 3C-PITC against mechanical hyperalgesia and spontaneous pain induced by nerve injury and osteoarthritis. METHODS: Nerve injury and osteoarthritis were induced in rats by ligation of the sciatic nerve (chronic constriction injury) and intra-articular injection of monoiodoacetate, respectively. Behavioral tests were performed 14 days after damage induction. RESULTS: Single subcutaneous administrations of PITC, 3C-PITC (4.43 and 13.31 µmol kg(−1), respectively) were able to completely reverse hypersensitivity to noxious stimuli in both models of neuropathic and osteoarticular pain. The effect of ITCs was compared with that of NaHS, the prototypical H(2)S donor, showing similar efficacy and higher potency. ITCs and NaHS also reduced spontaneous pain. CONCLUSION: ITCs offer a promising novel approach to counteract persistent, drug-resistant painful pathology. |
format | Online Article Text |
id | pubmed-6250104 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-62501042018-12-03 Efficacy of isothiocyanate-based compounds on different forms of persistent pain Lucarini, Elena Micheli, Laura Martelli, Alma Testai, Lara Calderone, Vincenzo Ghelardini, Carla Di Cesare Mannelli, Lorenzo J Pain Res Original Research PURPOSE: Current pharmacotherapy for persistent pain related to neuropathy or articular diseases is unsatisfactory, due to the large number of unresponsive patients and side effects. Isothiocyanates (ITCs) are a class of natural or synthetic compounds characterized by the general formula R–NCS. ITCs show antihyperalgesic effects in models of central and peripheral nervous tissue injury and anti-inflammatory properties. The pharmacodynamics are strictly related to the release of the gasotransmitter hydrogen sulfide (H(2)S) from their moiety. In particular, phenyl ITC (PITC) and 3-carboxyphenyl ITC (3C-PITC) exhibit interesting slow H(2)S-release properties suitable for treating painful pathology. The aim of the present work was to evaluate the efficacy of PITC and 3C-PITC against mechanical hyperalgesia and spontaneous pain induced by nerve injury and osteoarthritis. METHODS: Nerve injury and osteoarthritis were induced in rats by ligation of the sciatic nerve (chronic constriction injury) and intra-articular injection of monoiodoacetate, respectively. Behavioral tests were performed 14 days after damage induction. RESULTS: Single subcutaneous administrations of PITC, 3C-PITC (4.43 and 13.31 µmol kg(−1), respectively) were able to completely reverse hypersensitivity to noxious stimuli in both models of neuropathic and osteoarticular pain. The effect of ITCs was compared with that of NaHS, the prototypical H(2)S donor, showing similar efficacy and higher potency. ITCs and NaHS also reduced spontaneous pain. CONCLUSION: ITCs offer a promising novel approach to counteract persistent, drug-resistant painful pathology. Dove Medical Press 2018-11-19 /pmc/articles/PMC6250104/ /pubmed/30510445 http://dx.doi.org/10.2147/JPR.S161882 Text en © 2018 Lucarini et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Original Research Lucarini, Elena Micheli, Laura Martelli, Alma Testai, Lara Calderone, Vincenzo Ghelardini, Carla Di Cesare Mannelli, Lorenzo Efficacy of isothiocyanate-based compounds on different forms of persistent pain |
title | Efficacy of isothiocyanate-based compounds on different forms of persistent pain |
title_full | Efficacy of isothiocyanate-based compounds on different forms of persistent pain |
title_fullStr | Efficacy of isothiocyanate-based compounds on different forms of persistent pain |
title_full_unstemmed | Efficacy of isothiocyanate-based compounds on different forms of persistent pain |
title_short | Efficacy of isothiocyanate-based compounds on different forms of persistent pain |
title_sort | efficacy of isothiocyanate-based compounds on different forms of persistent pain |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6250104/ https://www.ncbi.nlm.nih.gov/pubmed/30510445 http://dx.doi.org/10.2147/JPR.S161882 |
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