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Synthesis of new 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives and evaluation for their 5-HT and D receptor affinity and serotonin transporter inhibition

2020
journal article
article
10.1016/j.bioorg.2020.103662
Journal
Bioorganic Chemistry
100
Author
Wróbel Martyna Z.

Chodkowski Andrzej

Marciniak Monika

Dawidowski Maciej

Maksymiuk Anna
Show more
Volume
97
Article ID
103662
ISSN
0045-2068
eISSN
1090-2120
Keywords in English

long-chain arylpiperazines

depression

5-HT receptor ligands

schizophrenia

multi-target ligands

Language
English
Journal language
English
Abstract in English

A series of novel 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives were synthesized and evaluated for their 5-HT/D2 receptor affinity and serotonin reuptake inhibition. The compounds exhibited high affinity for the 5-HT receptor, (especially 4d K = 0.4 nM) which depended on the substitution pattern at the phenylpiperazine moiety. From this series screen, compound 4c emerged with promising mixed receptor profiles for the 5-HT/D2 receptors and the serotonin transporter (K = 1.3 nM, 182 nM and 64 nM, respectively).

long-chain arylpiperazines

depression

5-HT receptor ligands

schizophrenia

multi-target ligands

Affiliation
Wydział Farmaceutyczny : Katedra FarmakobiologiiWydział Farmaceutyczny : Zakład Cytobiologii
Scopus© citations
13
cris.lastimport.wos2024-04-09T22:55:28Z
dc.abstract.enA series of novel 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives were synthesized and evaluated for their 5-HT$_{1A}$/D2 receptor affinity and serotonin reuptake inhibition. The compounds exhibited high affinity for the 5-HT$_{1A}$ receptor, (especially 4d K$_{i}$ = 0.4 nM) which depended on the substitution pattern at the phenylpiperazine moiety. From this series screen, compound 4c emerged with promising mixed receptor profiles for the 5-HT$_{1A}$/D2 receptors and the serotonin transporter (K$_{i}$ = 1.3 nM, 182 nM and 64 nM, respectively).pl
dc.abstract.enlong-chain arylpiperazinespl
dc.abstract.endepressionpl
dc.abstract.en5-HT$_{1A}$ receptor ligandspl
dc.abstract.enschizophreniapl
dc.abstract.enmulti-target ligandspl
dc.affiliationWydział Farmaceutyczny : Katedra Farmakobiologiipl
dc.affiliationWydział Farmaceutyczny : Zakład Cytobiologiipl
dc.cm.date2020-12-02
dc.cm.id98847
dc.contributor.authorWróbel, Martyna Z.pl
dc.contributor.authorChodkowski, Andrzejpl
dc.contributor.authorMarciniak, Monikapl
dc.contributor.authorDawidowski, Maciejpl
dc.contributor.authorMaksymiuk, Annapl
dc.contributor.authorSiwek, Agata - 133399 pl
dc.contributor.authorNowak, Gabriel - 132996 pl
dc.contributor.authorTurło, Jadwigapl
dc.date.accessioned2020-12-02T10:25:36Zpl
dc.date.available2020-12-02T10:25:36Zpl
dc.date.issued2020pl
dc.date.openaccess0
dc.description.accesstimew momencie opublikowania
dc.description.points100pl
dc.description.versionostateczna wersja wydawcy
dc.description.volume97pl
dc.identifier.articleid103662pl
dc.identifier.doi10.1016/j.bioorg.2020.103662pl
dc.identifier.eissn1090-2120pl
dc.identifier.issn0045-2068pl
dc.identifier.projectROD UJ / OPpl
dc.identifier.urihttps://ruj.uj.edu.pl/xmlui/handle/item/257359
dc.languageengpl
dc.language.containerengpl
dc.rightsUdzielam licencji. Uznanie autorstwa - Użycie niekomercyjne - Bez utworów zależnych 4.0 Międzynarodowa*
dc.rights.licenceCC-BY
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/pl/legalcode *
dc.share.typeotwarte czasopismo
dc.subject.enlong-chain arylpiperazinespl
dc.subject.endepressionpl
dc.subject.en5-HT$_{1A}$ receptor ligandspl
dc.subject.enschizophreniapl
dc.subject.enmulti-target ligandspl
dc.subtypeArticlepl
dc.titleSynthesis of new 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives and evaluation for their 5-HT$_{1A}$ and D$_{2}$ receptor affinity and serotonin transporter inhibitionpl
dc.title.journalBioorganic Chemistrypl
dc.typeJournalArticlepl
dspace.entity.typePublication
cris.lastimport.wos
2024-04-09T22:55:28Z
dc.abstract.enpl
A series of novel 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives were synthesized and evaluated for their 5-HT$_{1A}$/D2 receptor affinity and serotonin reuptake inhibition. The compounds exhibited high affinity for the 5-HT$_{1A}$ receptor, (especially 4d K$_{i}$ = 0.4 nM) which depended on the substitution pattern at the phenylpiperazine moiety. From this series screen, compound 4c emerged with promising mixed receptor profiles for the 5-HT$_{1A}$/D2 receptors and the serotonin transporter (K$_{i}$ = 1.3 nM, 182 nM and 64 nM, respectively).
dc.abstract.enpl
long-chain arylpiperazines
dc.abstract.enpl
depression
dc.abstract.enpl
5-HT$_{1A}$ receptor ligands
dc.abstract.enpl
schizophrenia
dc.abstract.enpl
multi-target ligands
dc.affiliationpl
Wydział Farmaceutyczny : Katedra Farmakobiologii
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Cytobiologii
dc.cm.date
2020-12-02
dc.cm.id
98847
dc.contributor.authorpl
Wróbel, Martyna Z.
dc.contributor.authorpl
Chodkowski, Andrzej
dc.contributor.authorpl
Marciniak, Monika
dc.contributor.authorpl
Dawidowski, Maciej
dc.contributor.authorpl
Maksymiuk, Anna
dc.contributor.authorpl
Siwek, Agata - 133399
dc.contributor.authorpl
Nowak, Gabriel - 132996
dc.contributor.authorpl
Turło, Jadwiga
dc.date.accessionedpl
2020-12-02T10:25:36Z
dc.date.availablepl
2020-12-02T10:25:36Z
dc.date.issuedpl
2020
dc.date.openaccess
0
dc.description.accesstime
w momencie opublikowania
dc.description.pointspl
100
dc.description.version
ostateczna wersja wydawcy
dc.description.volumepl
97
dc.identifier.articleidpl
103662
dc.identifier.doipl
10.1016/j.bioorg.2020.103662
dc.identifier.eissnpl
1090-2120
dc.identifier.issnpl
0045-2068
dc.identifier.projectpl
ROD UJ / OP
dc.identifier.uri
https://ruj.uj.edu.pl/xmlui/handle/item/257359
dc.languagepl
eng
dc.language.containerpl
eng
dc.rights*
Udzielam licencji. Uznanie autorstwa - Użycie niekomercyjne - Bez utworów zależnych 4.0 Międzynarodowa
dc.rights.licence
CC-BY
dc.rights.uri*
http://creativecommons.org/licenses/by-nc-nd/4.0/pl/legalcode 
dc.share.type
otwarte czasopismo
dc.subject.enpl
long-chain arylpiperazines
dc.subject.enpl
depression
dc.subject.enpl
5-HT$_{1A}$ receptor ligands
dc.subject.enpl
schizophrenia
dc.subject.enpl
multi-target ligands
dc.subtypepl
Article
dc.titlepl
Synthesis of new 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives and evaluation for their 5-HT$_{1A}$ and D$_{2}$ receptor affinity and serotonin transporter inhibition
dc.title.journalpl
Bioorganic Chemistry
dc.typepl
JournalArticle
dspace.entity.type
Publication
Affiliations
Wydział Farmaceutyczny
Siwek, Agata
Nowak, Gabriel
No affiliation
Wróbel, Martyna Z.
Chodkowski, Andrzej
Marciniak, Monika
Dawidowski, Maciej
Maksymiuk, Anna
Turło, Jadwiga

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