Potential anti-amnesic activity of a novel multimodal derivative of salicylamide, JJGW08, in mice

2023
journal article
article
2
dc.abstract.enMemory impairments constitute a significant problem worldwide, and the COVID-19 pandemic dramatically increased the prevalence of cognitive deficits. Patients with cognitive deficits, specifically memory disturbances, have underlying comorbid conditions such as schizophrenia, anxiety, or depression. Moreover, the available treatment options have unsatisfactory effectiveness. Therefore, there is a need to search for novel procognitive and anti-amnesic drugs with additional pharmacological activity. One of the important therapeutic targets involved in the modulation of learning and memory processes are serotonin receptors, including 5-HT$_{1A}$, 5-HT$_{6}$, and 5-HT$_{7}$, which also play a role in the pathophysiology of depression. Therefore, this study aimed to assess the anti-amnesic and antidepressant-like potential of JJGW08, a novel arylpiperazine alkyl derivative of salicylamide with strong antagonistic properties at 5-HT$_{1A}$ and D$_{2}$ receptors and weak at 5-HT$_{2A}$ and 5-HT$_{7}$ receptors in rodents. First, we investigated the compound’s affinity for 5-HT$_{61A}$ receptors using the radioligand assays. Next, we assessed the influence of the compound on long-term emotional and recognition memory. Further, we evaluated whether the compound could protect against MK-801-induced cognitive impairments. Finally, we determined the potential antidepressant-like activity of the tested compound. We found that JJGW08 possessed no affinity for 5-HT$_{6}$ receptors. Furthermore, JJGW08 protected mice against MK-801-induced recognition and emotional memory deficits but showed no antidepressant-like effects in rodents. Therefore, our preliminary study may suggest that blocking serotonin receptors, especially 5-HT$_{1A}$ and 5-HT$_{7}$, might be beneficial in treating cognitive impairments, but it requires further investigation.
dc.affiliationWydział Farmaceutyczny : Zakład Chemii Lekówpl
dc.affiliationWydział Farmaceutyczny : Zakład Wstępnych Badań Farmakologicznychpl
dc.affiliationWydział Farmaceutyczny : Zakład Farmacji Społecznejpl
dc.affiliationWydział Farmaceutyczny : Zakład Radioligandówpl
dc.affiliationWydział Farmaceutyczny : Zakład Farmakodynamikipl
dc.cm.date2023-04-26T22:17:30Z
dc.cm.id111887pl
dc.cm.idOmegaUJCM85efc11586b941c69b2d5c0e54504c9dpl
dc.contributor.authorŻmudzka, Elżbieta - 163801 pl
dc.contributor.authorLustyk, Klaudia - 151709 pl
dc.contributor.authorSałaciak, Kinga - 215739 pl
dc.contributor.authorSiwek, Agata - 133399 pl
dc.contributor.authorJaśkowska, Jolantapl
dc.contributor.authorKołaczkowski, Marcin - 130216 pl
dc.contributor.authorSapa, Jacek - 133358 pl
dc.contributor.authorPytka, Karolina - 140569 pl
dc.date.accession2023-04-26pl
dc.date.accessioned2023-04-26T22:17:30Z
dc.date.available2023-04-26T22:17:30Z
dc.date.issued2023pl
dc.date.openaccess0
dc.description.accesstimew momencie opublikowania
dc.description.number3pl
dc.description.versionostateczna wersja wydawcy
dc.description.volume16pl
dc.identifier.articleid399pl
dc.identifier.doi10.3390/ph16030399pl
dc.identifier.eissn1424-8247pl
dc.identifier.issn1424-8247pl
dc.identifier.urihttps://ruj.uj.edu.pl/xmlui/handle/item/310870
dc.identifier.weblinkhttps://www.mdpi.com/1424-8247/16/3/399pl
dc.languageengpl
dc.language.containerengpl
dc.pbn.affiliationDziedzina nauk medycznych i nauk o zdrowiu : nauki farmaceutyczne
dc.rightsUdzielam licencji. Uznanie autorstwa 4.0 Międzynarodowa
dc.rights.licenceCC-BY
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/legalcode.pl
dc.share.typeOtwarte czasopismo
dc.subject.enanti-amnesic effect
dc.subject.enlong-term memory
dc.subject.encognition
dc.subject.enantidepressant-like activity
dc.subject.enserotonin receptors
dc.subtypeArticlepl
dc.titlePotential anti-amnesic activity of a novel multimodal derivative of salicylamide, JJGW08, in micepl
dc.title.journalPharmaceuticalspl
dc.typeJournalArticlepl
dspace.entity.typePublication
dc.abstract.en
Memory impairments constitute a significant problem worldwide, and the COVID-19 pandemic dramatically increased the prevalence of cognitive deficits. Patients with cognitive deficits, specifically memory disturbances, have underlying comorbid conditions such as schizophrenia, anxiety, or depression. Moreover, the available treatment options have unsatisfactory effectiveness. Therefore, there is a need to search for novel procognitive and anti-amnesic drugs with additional pharmacological activity. One of the important therapeutic targets involved in the modulation of learning and memory processes are serotonin receptors, including 5-HT$_{1A}$, 5-HT$_{6}$, and 5-HT$_{7}$, which also play a role in the pathophysiology of depression. Therefore, this study aimed to assess the anti-amnesic and antidepressant-like potential of JJGW08, a novel arylpiperazine alkyl derivative of salicylamide with strong antagonistic properties at 5-HT$_{1A}$ and D$_{2}$ receptors and weak at 5-HT$_{2A}$ and 5-HT$_{7}$ receptors in rodents. First, we investigated the compound’s affinity for 5-HT$_{61A}$ receptors using the radioligand assays. Next, we assessed the influence of the compound on long-term emotional and recognition memory. Further, we evaluated whether the compound could protect against MK-801-induced cognitive impairments. Finally, we determined the potential antidepressant-like activity of the tested compound. We found that JJGW08 possessed no affinity for 5-HT$_{6}$ receptors. Furthermore, JJGW08 protected mice against MK-801-induced recognition and emotional memory deficits but showed no antidepressant-like effects in rodents. Therefore, our preliminary study may suggest that blocking serotonin receptors, especially 5-HT$_{1A}$ and 5-HT$_{7}$, might be beneficial in treating cognitive impairments, but it requires further investigation.
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Chemii Leków
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Wstępnych Badań Farmakologicznych
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Farmacji Społecznej
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Radioligandów
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Farmakodynamiki
dc.cm.date
2023-04-26T22:17:30Z
dc.cm.idpl
111887
dc.cm.idOmegapl
UJCM85efc11586b941c69b2d5c0e54504c9d
dc.contributor.authorpl
Żmudzka, Elżbieta - 163801
dc.contributor.authorpl
Lustyk, Klaudia - 151709
dc.contributor.authorpl
Sałaciak, Kinga - 215739
dc.contributor.authorpl
Siwek, Agata - 133399
dc.contributor.authorpl
Jaśkowska, Jolanta
dc.contributor.authorpl
Kołaczkowski, Marcin - 130216
dc.contributor.authorpl
Sapa, Jacek - 133358
dc.contributor.authorpl
Pytka, Karolina - 140569
dc.date.accessionpl
2023-04-26
dc.date.accessioned
2023-04-26T22:17:30Z
dc.date.available
2023-04-26T22:17:30Z
dc.date.issuedpl
2023
dc.date.openaccess
0
dc.description.accesstime
w momencie opublikowania
dc.description.numberpl
3
dc.description.version
ostateczna wersja wydawcy
dc.description.volumepl
16
dc.identifier.articleidpl
399
dc.identifier.doipl
10.3390/ph16030399
dc.identifier.eissnpl
1424-8247
dc.identifier.issnpl
1424-8247
dc.identifier.uri
https://ruj.uj.edu.pl/xmlui/handle/item/310870
dc.identifier.weblinkpl
https://www.mdpi.com/1424-8247/16/3/399
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
Otwarte czasopismo
dc.subject.en
anti-amnesic effect
dc.subject.en
long-term memory
dc.subject.en
cognition
dc.subject.en
antidepressant-like activity
dc.subject.en
serotonin receptors
dc.subtypepl
Article
dc.titlepl
Potential anti-amnesic activity of a novel multimodal derivative of salicylamide, JJGW08, in mice
dc.title.journalpl
Pharmaceuticals
dc.typepl
JournalArticle
dspace.entity.type
Publication
Affiliations

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