Differential activity of decynium-22 analogs: novel targets for probing low-affinity/high-capacity biogenic amine transporters

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dc.contributor.authorFraser, Ren_AU
dc.contributor.authorOwens, Aen_AU
dc.contributor.authorWyatt, NAen_AU
dc.contributor.authorKrause-Heuer, AMen_AU
dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorCallaghan, PDen_AU
dc.contributor.authorFraser, BHen_AU
dc.contributor.authorDaws, LCen_AU
dc.date.accessioned2021-08-11T05:06:47Zen_AU
dc.date.available2021-08-11T05:06:47Zen_AU
dc.date.issued2015-04-01en_AU
dc.date.statistics2021-08-10en_AU
dc.description.abstractWe study neurotransmitter clearance by low-affinity, high-capacity uptake-2 transporters. This family includes plasma membrane monoamine transporter (PMAT) and three organic cation transporter isoforms (OCT1-3). We have shown uptake-2 transporters limit the effectiveness of the selective serotonin reuptake inhibitor (SSRI) fluvoxamine. Discerning the transporter type(s) involved is restricted by the lack of highly selective ligands. This project examines the pharmacological characteristics of novel uptake-2 compounds. Activity of ANSTO analogs, structurally based on the non-selective inhibitor decynium 22 (D22), was tested in human OCT3-HEK cells. Ligand competitions of [3H]MPP+ uptake were measured in whole, attached cells. Compared to D22, dose-responses of ANSTO compounds shifted 1- or 2 log-rightward, indicating reduced potency to inhibit OCT3 mediated [3H]MPP+ uptake. ANSTO analogs displayed similar potencies to corticosterone and may have higher selectivity at alternate uptake 2 subtypes. © 2015 Federation of American Societies for Experimental Biology (FASEB)en_AU
dc.identifier.citationFraser, R., Owens, W. A., Wyatt, N., Krause-Heuer, A., Greguric, I., Callaghan, P., Fraser, B., & Daws, L. (2015). Differential activity of decynium-22 analogs: novel targets for probing low-affinity/high-capacity biogenic amine transporters. The FASEB Journal, 29(S1), 932.934. doi:10.1096/fasebj.29.1_supplement.932.4en_AU
dc.identifier.issn1530-6860en_AU
dc.identifier.issueS1en_AU
dc.identifier.journaltitleThe FASEB Journalen_AU
dc.identifier.pagination932.4en_AU
dc.identifier.urihttps://doi.org/10.1096/fasebj.29.1_supplement.932.4en_AU
dc.identifier.urihttps://apo.ansto.gov.au/dspace/handle/10238/11325en_AU
dc.identifier.volume29en_AU
dc.language.isoenen_AU
dc.publisherFederation of American Societies for Experimental Biology (FASEB)en_AU
dc.subjectMembranesen_AU
dc.subjectCationsen_AU
dc.subjectSerotoninen_AU
dc.subjectEnzyme inhibitorsen_AU
dc.subjectPharmacologyen_AU
dc.subjectLigandsen_AU
dc.titleDifferential activity of decynium-22 analogs: novel targets for probing low-affinity/high-capacity biogenic amine transportersen_AU
dc.typeJournal Articleen_AU
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