A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice

OBJECTIVE: 5-HOB is a novel tissue selective, 5-hydroxybenzothiazolone-derived β2 adrenoceptor agonist with minimized cardiovascular effects while retaining efficacy on skeletal muscle in preclinical experiments unlike conventional β2 adrenoceptor agonists, however its effect on the nervous system h...

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Detalles Bibliográficos
Autores principales: Jourdain, Marie, Hatakeyama, Shinji
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2019
Materias:
Research Note
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6632195/
https://www.ncbi.nlm.nih.gov/pubmed/31307541
http://dx.doi.org/10.1186/s13104-019-4466-y
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author Jourdain, Marie
Hatakeyama, Shinji
author_facet Jourdain, Marie
Hatakeyama, Shinji
author_sort Jourdain, Marie
collection PubMed
description OBJECTIVE: 5-HOB is a novel tissue selective, 5-hydroxybenzothiazolone-derived β2 adrenoceptor agonist with minimized cardiovascular effects while retaining efficacy on skeletal muscle in preclinical experiments unlike conventional β2 adrenoceptor agonists, however its effect on the nervous system has not been evaluated yet. Therefore, 5-HOB was evaluated in a mouse model of neuropathic pain. RESULTS: 5-HOB alleviated neuropathic allodynia in a dose dependent manner and reversed the changes in hind paw withdrawal thresholds to the sham control levels. The dose attenuating neuropathic allodynia was slightly lower than the dose inducing skeletal muscle hypertrophy. In conclusion, as reported with known β2 adrenoceptor agonists, 5-HOB was also effective in attenuating neuropathic pain in mice in addition to its effect on skeletal muscle.
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spelling pubmed-66321952019-07-25 A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice Jourdain, Marie Hatakeyama, Shinji BMC Res Notes Research Note OBJECTIVE: 5-HOB is a novel tissue selective, 5-hydroxybenzothiazolone-derived β2 adrenoceptor agonist with minimized cardiovascular effects while retaining efficacy on skeletal muscle in preclinical experiments unlike conventional β2 adrenoceptor agonists, however its effect on the nervous system has not been evaluated yet. Therefore, 5-HOB was evaluated in a mouse model of neuropathic pain. RESULTS: 5-HOB alleviated neuropathic allodynia in a dose dependent manner and reversed the changes in hind paw withdrawal thresholds to the sham control levels. The dose attenuating neuropathic allodynia was slightly lower than the dose inducing skeletal muscle hypertrophy. In conclusion, as reported with known β2 adrenoceptor agonists, 5-HOB was also effective in attenuating neuropathic pain in mice in addition to its effect on skeletal muscle. BioMed Central 2019-07-15 /pmc/articles/PMC6632195/ /pubmed/31307541 http://dx.doi.org/10.1186/s13104-019-4466-y Text en © The Author(s) 2019 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research Note
Jourdain, Marie
Hatakeyama, Shinji
A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice
title A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice
title_full A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice
title_fullStr A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice
title_full_unstemmed A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice
title_short A novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-HOB, attenuates neuropathic pain in mice
title_sort novel tissue-selective β2-adrenoceptor agonist with minimized cardiovascular effects, 5-hob, attenuates neuropathic pain in mice
topic Research Note
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6632195/
https://www.ncbi.nlm.nih.gov/pubmed/31307541
http://dx.doi.org/10.1186/s13104-019-4466-y
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