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RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice

Treatment of pain and fever remains an important challenge for modern medicine. Non-steroidal anti-inflammatory drugs (NSAIDs) are the pharmacological options most often used, but their frequent use exposes the patient to serious side effects and dangerous drug interactions. In this context, thiophe...

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Autores principales: da Cruz, Ryldene Marques Duarte, Braga, Renan Marinho, de Andrade, Humberto Hugo Nunes, Monteiro, Álefe Brito, Luna, Isadora Silva, da Cruz, Rayssa Marques Duarte, Scotti, Marcus Tullius, Mendonça-Junior, Francisco Jaime Bezerra, de Almeida, Reinaldo Nóbrega
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7695913/
https://www.ncbi.nlm.nih.gov/pubmed/33294672
http://dx.doi.org/10.1016/j.heliyon.2020.e05520
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author da Cruz, Ryldene Marques Duarte
Braga, Renan Marinho
de Andrade, Humberto Hugo Nunes
Monteiro, Álefe Brito
Luna, Isadora Silva
da Cruz, Rayssa Marques Duarte
Scotti, Marcus Tullius
Mendonça-Junior, Francisco Jaime Bezerra
de Almeida, Reinaldo Nóbrega
author_facet da Cruz, Ryldene Marques Duarte
Braga, Renan Marinho
de Andrade, Humberto Hugo Nunes
Monteiro, Álefe Brito
Luna, Isadora Silva
da Cruz, Rayssa Marques Duarte
Scotti, Marcus Tullius
Mendonça-Junior, Francisco Jaime Bezerra
de Almeida, Reinaldo Nóbrega
author_sort da Cruz, Ryldene Marques Duarte
collection PubMed
description Treatment of pain and fever remains an important challenge for modern medicine. Non-steroidal anti-inflammatory drugs (NSAIDs) are the pharmacological options most often used, but their frequent use exposes the patient to serious side effects and dangerous drug interactions. In this context, thiophene derivatives are promising therapeutic alternatives. In this study, we evaluated the in vivo and in silico antinociceptive and antipyretic properties of RMD86, a thiophene derivative. At 100 mg/kg, RMD86 induced no significant changes in the motor coordination of mice in the Rotarod test. At 25, 50, and 100 mg/kg RMD86 significantly reduced the number of abdominal contortions induced by acetic acid (antinociceptive activity) in mice when compared to the control. In the formalin test, for the first phase, there was a reduction in licking times at doses of 50 and 100 mg/kg. In the second phase, reduction occurred at all doses. In the hot plate test, RMD86 (at 100 mg/kg) increased latency time in the first 30 min. For antipyretic activity, RMD86, when compared to the reference drug acetaminophen (250 mg/kg), significantly reduced pyrexia at 30, 60, and 120 min, at dosages of 25, 50 and 100 mg/kg. Molecular docking studies revealed that RMD86 presents a greater number of interactions and lower energy values than both the co-crystallized ligand and the reference drug (meloxicam) against COX-1 and COX-2 isoenzymes. The results give evidence of the analgesic and antipyretic properties like NSAIDs suggesting its potential for pain therapy.
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spelling pubmed-76959132020-12-07 RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice da Cruz, Ryldene Marques Duarte Braga, Renan Marinho de Andrade, Humberto Hugo Nunes Monteiro, Álefe Brito Luna, Isadora Silva da Cruz, Rayssa Marques Duarte Scotti, Marcus Tullius Mendonça-Junior, Francisco Jaime Bezerra de Almeida, Reinaldo Nóbrega Heliyon Research Article Treatment of pain and fever remains an important challenge for modern medicine. Non-steroidal anti-inflammatory drugs (NSAIDs) are the pharmacological options most often used, but their frequent use exposes the patient to serious side effects and dangerous drug interactions. In this context, thiophene derivatives are promising therapeutic alternatives. In this study, we evaluated the in vivo and in silico antinociceptive and antipyretic properties of RMD86, a thiophene derivative. At 100 mg/kg, RMD86 induced no significant changes in the motor coordination of mice in the Rotarod test. At 25, 50, and 100 mg/kg RMD86 significantly reduced the number of abdominal contortions induced by acetic acid (antinociceptive activity) in mice when compared to the control. In the formalin test, for the first phase, there was a reduction in licking times at doses of 50 and 100 mg/kg. In the second phase, reduction occurred at all doses. In the hot plate test, RMD86 (at 100 mg/kg) increased latency time in the first 30 min. For antipyretic activity, RMD86, when compared to the reference drug acetaminophen (250 mg/kg), significantly reduced pyrexia at 30, 60, and 120 min, at dosages of 25, 50 and 100 mg/kg. Molecular docking studies revealed that RMD86 presents a greater number of interactions and lower energy values than both the co-crystallized ligand and the reference drug (meloxicam) against COX-1 and COX-2 isoenzymes. The results give evidence of the analgesic and antipyretic properties like NSAIDs suggesting its potential for pain therapy. Elsevier 2020-11-23 /pmc/articles/PMC7695913/ /pubmed/33294672 http://dx.doi.org/10.1016/j.heliyon.2020.e05520 Text en © 2020 Published by Elsevier Ltd. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Research Article
da Cruz, Ryldene Marques Duarte
Braga, Renan Marinho
de Andrade, Humberto Hugo Nunes
Monteiro, Álefe Brito
Luna, Isadora Silva
da Cruz, Rayssa Marques Duarte
Scotti, Marcus Tullius
Mendonça-Junior, Francisco Jaime Bezerra
de Almeida, Reinaldo Nóbrega
RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice
title RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice
title_full RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice
title_fullStr RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice
title_full_unstemmed RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice
title_short RMD86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice
title_sort rmd86, a thiophene derivative, promotes antinociceptive and antipyretic activities in mice
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7695913/
https://www.ncbi.nlm.nih.gov/pubmed/33294672
http://dx.doi.org/10.1016/j.heliyon.2020.e05520
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