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Evaluation of analgesic and anti-inflammatory activity of purine-2,6-dione-based TRPA1 antagonists with PDE4/7 inhibitory activity
Journal
Pharmacological Reports
100
Author
Volume
74
Number
5
Pages
982-997
ISSN
1734-1140
eISSN
2299-5684
Keywords in English
purine-2
6-diones
trpa1 antagonists
pde4/7 inhibitors
analgesic activity
anti-inflammatory activity
antiarthritic effect
Access date
2022-08-20
Remarks
Online First 2022-08-05
Language
English
Journal language
English
Abstract in English
Background: To verify the validity of the proposed pain treatment approach, which is based on concomitant blocking of the Transient Receptor Potential Ankyrin 1 (TRPA1) channel and phosphodiesterases (PDEs) 4B/7A activity, we continued our pharmacological studies on 8-alkoxypurine-2,6-diones selected based on previous in vitro screening. Methods: Derivatives 17, 31, and 36 were pharmacologically evaluated in vivo using the formalin test and oxaliplatin-induced neuropathic pain: the von Frey and the cold plate tests, and in the carrageenan-induced edema model. Compound 36, which turned out to be the most promising, was further evaluated in the collagen-induced arthritis model. The pharmacokinetic parameters of this compound were also estimated. Results: All the tested compounds exhibited significant analgesic and anti-inflammatory activities. Compound 36 was additionally characterized by an antiarthritic effect and showed a favorable pharmacokinetic profile in rats. Conclusion: The compounds evaluated in this study represent a new class of derivatives with analgesic and anti-inflammatory activities that involve TRPA1 antagonism and PDE4/7 inhibition.
Affiliation
Wydział Farmaceutyczny : Zakład Chemii LekówWydział Farmaceutyczny : Zakład Wstępnych Badań FarmakologicznychWydział Farmaceutyczny : Zakład Farmakokinetyki i Farmacji FizycznejWydział Farmaceutyczny : Zakład Farmakodynamiki
Scopus© citations
5
| cris.lastimport.wos | 2024-04-10T00:02:59Z | |
| dc.abstract.en | Background: To verify the validity of the proposed pain treatment approach, which is based on concomitant blocking of the Transient Receptor Potential Ankyrin 1 (TRPA1) channel and phosphodiesterases (PDEs) 4B/7A activity, we continued our pharmacological studies on 8-alkoxypurine-2,6-diones selected based on previous in vitro screening. Methods: Derivatives 17, 31, and 36 were pharmacologically evaluated in vivo using the formalin test and oxaliplatin-induced neuropathic pain: the von Frey and the cold plate tests, and in the carrageenan-induced edema model. Compound 36, which turned out to be the most promising, was further evaluated in the collagen-induced arthritis model. The pharmacokinetic parameters of this compound were also estimated. Results: All the tested compounds exhibited significant analgesic and anti-inflammatory activities. Compound 36 was additionally characterized by an antiarthritic effect and showed a favorable pharmacokinetic profile in rats. Conclusion: The compounds evaluated in this study represent a new class of derivatives with analgesic and anti-inflammatory activities that involve TRPA1 antagonism and PDE4/7 inhibition. | |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Chemii Leków | pl |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Wstępnych Badań Farmakologicznych | pl |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Farmakokinetyki i Farmacji Fizycznej | pl |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Farmakodynamiki | pl |
| dc.cm.date | 2022-08-22T05:32:48Z | |
| dc.cm.id | 109237 | pl |
| dc.cm.idOmega | UJCMaa851cd214d041de80b91fc8241ce8dd | pl |
| dc.contributor.author | Zygmunt, Małgorzata - 133939 | pl |
| dc.contributor.author | Ślusarczyk, Marietta | pl |
| dc.contributor.author | Jankowska, Agnieszka | pl |
| dc.contributor.author | Świerczek, Artur - 164021 | pl |
| dc.contributor.author | Bryła, Adrian | pl |
| dc.contributor.author | Mogilski, Szczepan - 131010 | pl |
| dc.contributor.author | Kazek, Grzegorz - 159986 | pl |
| dc.contributor.author | Sapa, Jacek - 133358 | pl |
| dc.contributor.author | Wyska, Elżbieta - 133861 | pl |
| dc.contributor.author | Chłoń-Rzepa, Grażyna - 128990 | pl |
| dc.date.accession | 2022-08-20 | pl |
| dc.date.accessioned | 2022-08-22T05:32:48Z | |
| dc.date.available | 2022-08-22T05:32:48Z | |
| dc.date.issued | 2022 | pl |
| dc.date.openaccess | 0 | |
| dc.description.accesstime | w momencie opublikowania | |
| dc.description.additional | Online First 2022-08-05 | pl |
| dc.description.number | 5 | pl |
| dc.description.physical | 982-997 | pl |
| dc.description.version | ostateczna wersja wydawcy | |
| dc.description.volume | 74 | pl |
| dc.identifier.doi | 10.1007/s43440-022-00397-6 | pl |
| dc.identifier.eissn | 2299-5684 | pl |
| dc.identifier.issn | 1734-1140 | pl |
| dc.identifier.uri | https://ruj.uj.edu.pl/xmlui/handle/item/298315 | |
| dc.identifier.weblink | https://link.springer.com/article/10.1007/s43440-022-00397-6 | pl |
| dc.language | eng | pl |
| dc.language.container | eng | pl |
| dc.pbn.affiliation | Dziedzina nauk medycznych i nauk o zdrowiu : nauki farmaceutyczne | |
| dc.rights | Udzielam licencji. Uznanie autorstwa 4.0 Międzynarodowa | |
| dc.rights.licence | CC-BY | |
| dc.rights.uri | http://creativecommons.org/licenses/by/4.0/legalcode.pl | |
| dc.share.type | inne | |
| dc.subject.en | purine-2 | |
| dc.subject.en | 6-diones | |
| dc.subject.en | trpa1 antagonists | |
| dc.subject.en | pde4/7 inhibitors | |
| dc.subject.en | analgesic activity | |
| dc.subject.en | anti-inflammatory activity | |
| dc.subject.en | antiarthritic effect | |
| dc.subtype | Article | pl |
| dc.title | Evaluation of analgesic and anti-inflammatory activity of purine-2,6-dione-based TRPA1 antagonists with PDE4/7 inhibitory activity | pl |
| dc.title.journal | Pharmacological Reports | pl |
| dc.type | JournalArticle | pl |
| dspace.entity.type | Publication |
cris.lastimport.wos
2024-04-10T00:02:59Z dc.abstract.en
Background: To verify the validity of the proposed pain treatment approach, which is based on concomitant blocking of the Transient Receptor Potential Ankyrin 1 (TRPA1) channel and phosphodiesterases (PDEs) 4B/7A activity, we continued our pharmacological studies on 8-alkoxypurine-2,6-diones selected based on previous in vitro screening. Methods: Derivatives 17, 31, and 36 were pharmacologically evaluated in vivo using the formalin test and oxaliplatin-induced neuropathic pain: the von Frey and the cold plate tests, and in the carrageenan-induced edema model. Compound 36, which turned out to be the most promising, was further evaluated in the collagen-induced arthritis model. The pharmacokinetic parameters of this compound were also estimated. Results: All the tested compounds exhibited significant analgesic and anti-inflammatory activities. Compound 36 was additionally characterized by an antiarthritic effect and showed a favorable pharmacokinetic profile in rats. Conclusion: The compounds evaluated in this study represent a new class of derivatives with analgesic and anti-inflammatory activities that involve TRPA1 antagonism and PDE4/7 inhibition. dc.affiliationpl
Wydział Farmaceutyczny : Zakład Chemii Leków dc.affiliationpl
Wydział Farmaceutyczny : Zakład Wstępnych Badań Farmakologicznych dc.affiliationpl
Wydział Farmaceutyczny : Zakład Farmakokinetyki i Farmacji Fizycznej dc.affiliationpl
Wydział Farmaceutyczny : Zakład Farmakodynamiki dc.cm.date
2022-08-22T05:32:48Z dc.cm.idpl
109237 dc.cm.idOmegapl
UJCMaa851cd214d041de80b91fc8241ce8dd dc.contributor.authorpl
Zygmunt, Małgorzata - 133939 dc.contributor.authorpl
Ślusarczyk, Marietta dc.contributor.authorpl
Jankowska, Agnieszka dc.contributor.authorpl
Świerczek, Artur - 164021 dc.contributor.authorpl
Bryła, Adrian dc.contributor.authorpl
Mogilski, Szczepan - 131010 dc.contributor.authorpl
Kazek, Grzegorz - 159986 dc.contributor.authorpl
Sapa, Jacek - 133358 dc.contributor.authorpl
Wyska, Elżbieta - 133861 dc.contributor.authorpl
Chłoń-Rzepa, Grażyna - 128990 dc.date.accessionpl
2022-08-20 dc.date.accessioned
2022-08-22T05:32:48Z dc.date.available
2022-08-22T05:32:48Z dc.date.issuedpl
2022 dc.date.openaccess
0 dc.description.accesstime
w momencie opublikowania dc.description.additionalpl
Online First 2022-08-05 dc.description.numberpl
5 dc.description.physicalpl
982-997 dc.description.version
ostateczna wersja wydawcy dc.description.volumepl
74 dc.identifier.doipl
10.1007/s43440-022-00397-6 dc.identifier.eissnpl
2299-5684 dc.identifier.issnpl
1734-1140 dc.identifier.uri
https://ruj.uj.edu.pl/xmlui/handle/item/298315 dc.identifier.weblinkpl
https://link.springer.com/article/10.1007/s43440-022-00397-6 dc.languagepl
eng dc.language.containerpl
eng dc.pbn.affiliation
Dziedzina nauk medycznych i nauk o zdrowiu : nauki farmaceutyczne dc.rights
Udzielam licencji. Uznanie autorstwa 4.0 Międzynarodowa dc.rights.licence
CC-BY dc.rights.uri
http://creativecommons.org/licenses/by/4.0/legalcode.pl dc.share.type
inne dc.subject.en
purine-2 dc.subject.en
6-diones dc.subject.en
trpa1 antagonists dc.subject.en
pde4/7 inhibitors dc.subject.en
analgesic activity dc.subject.en
anti-inflammatory activity dc.subject.en
antiarthritic effect dc.subtypepl
Article dc.titlepl
Evaluation of analgesic and anti-inflammatory activity of purine-2,6-dione-based TRPA1 antagonists with PDE4/7 inhibitory activity dc.title.journalpl
Pharmacological Reports dc.typepl
JournalArticle dspace.entity.type
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