Full metadata record

DC Field Value Language
dc.contributor.authorAhn Hyomin-
dc.contributor.authorKichul Park-
dc.contributor.authorDongyoung Kim-
dc.contributor.authorSung-Gil Chi-
dc.contributor.authorKee-Hyun Choi-
dc.contributor.authorHan, Seojung-
dc.contributor.authorSong, Chiman-
dc.date.accessioned2024-01-12T06:33:31Z-
dc.date.available2024-01-12T06:33:31Z-
dc.date.created2023-10-21-
dc.date.issued2023-10-
dc.identifier.issn2227-9059-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/79801-
dc.description.abstractMonoamine transporters, including dopamine, norepinephrine, and serotonin transporters (DAT, NET, and SERT, respectively), are important therapeutic targets due to their essential roles in the brain. To overcome the slow action of selective monoamine reuptake inhibitors, dual- or triple-acting inhibitors have been developed. Here, to examine whether combination treatments of selective reuptake inhibitors have synergistic effects, the pharmacological properties of DAT, NET, and SERT were investigated using the selective inhibitors of each transporter, which are vanoxerine, nisoxetine, and fluoxetine, respectively. Potencies were determined via fluorescence-based substrate uptake assays in the absence and presence of other inhibitors to test the multi-drug effects on individual transporters, resulting in antagonistic effects on DAT. In detail, fluoxetine resulted in a 1.6-fold increased IC50 value of vanoxerine for DAT, and nisoxetine produced a more drastic increase in the IC50 value by six folds. Furthermore, the effects of different inhibitors, specifically monovalent ions, were tested on DAT inhibition by vanoxerine. Interestingly, these ions also reduced vanoxerine potency in a similar manner. The homology models of DAT suggested a potential secondary inhibitor binding site that affects inhibition in an allosteric manner. These findings imply that the use of combination therapy with monoamine reuptake inhibitors should be approached cautiously, as antagonistic effects may occur.-
dc.languageEnglish-
dc.publisherMDPI AG-
dc.titleImplications for Combination Therapy of Selective Monoamine Reuptake Inhibitors on Dopamine Transporters-
dc.typeArticle-
dc.identifier.doi10.3390/biomedicines11102846-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBiomedicines, v.11, no.10-
dc.citation.titleBiomedicines-
dc.citation.volume11-
dc.citation.number10-
dc.description.isOpenAccessY-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid001094006100001-
dc.relation.journalWebOfScienceCategoryBiochemistry & Molecular Biology-
dc.relation.journalWebOfScienceCategoryMedicine, Research & Experimental-
dc.relation.journalWebOfScienceCategoryPharmacology & Pharmacy-
dc.relation.journalResearchAreaBiochemistry & Molecular Biology-
dc.relation.journalResearchAreaResearch & Experimental Medicine-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.type.docTypeArticle-
dc.subject.keywordPlusBACTERIAL HOMOLOG-
dc.subject.keywordPlusUPTAKE BLOCKERS-
dc.subject.keywordPlusRAT-BRAIN-
dc.subject.keywordPlusBINDING-
dc.subject.keywordPlusSEROTONIN-
dc.subject.keywordPlusCHOLINE-
dc.subject.keywordPlusCOCAINE-
dc.subject.keywordPlusCATIONS-
dc.subject.keywordPlusNA+-
dc.subject.keywordAuthorantagonistic effect-
dc.subject.keywordAuthorvanoxerine-
dc.subject.keywordAuthornisoxetine-
dc.subject.keywordAuthorfluoxetine-
dc.subject.keywordAuthormonoamine transporter-
dc.subject.keywordAuthordopamine transporter-
Appears in Collections:
KIST Article > 2023
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML

qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE