Characterization of ligand binding to Dopamine D3 receptor using fluorescence anisotropy and radioligand binding

dc.contributor.authorThoondee, Lakshmi
dc.contributor.otherTartu Ülikool. Loodus- ja täppisteaduste valdkondet
dc.contributor.otherTartu Ülikool. Tehnoloogiainstituutet
dc.date.accessioned2021-07-01T11:42:12Z
dc.date.available2021-07-01T11:42:12Z
dc.date.issued2021
dc.description.abstractThere are five subtypes of dopamine receptors that play a role in the dopaminergic system. Due to their limited distribution and involvement in cognitive and emotional functions, Dopamine D3 receptors are attractive pharmacological targets for treatment of drug addiction and neuropsychiatric disorders. D3 receptor ligands have been labelled with a fluorescent dye or a radioisotope for direct monitoring of ligand binding to the receptor. However, there are not many fluorescent ligands that are available for studying D3 receptor. A2-TAMRA is a novel fluorescent ligand with high affinity for D3 receptor. Binding of [3H]-methylspiperone to D3R was studied in parallel to validate results from A2-TAMRA binding to D3R. The D3 receptor ligands had similar affinities in inhibiting A2-TAMRA and [3H]-methyl spiperone binding to D3 receptor, since a very good correlation (R2 = 0.94) was obtained between both methods. The affinities for the known antagonists had a good correlation with previously published data. Selectivity of A2-TAMRA towards two different subtypes was also studied and we found that A2-TAMRA prefers D3 receptor over D1 receptor.et
dc.identifier.urihttp://hdl.handle.net/10062/72924
dc.language.isoenget
dc.publisherTartu Ülikoolet
dc.rightsopenAccesset
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectdopamine receptorset
dc.subjectfluorescent ligandet
dc.subjectfluorescence anisotropy assayet
dc.subjectradioligand binding assayet
dc.subject.othermagistritöödet
dc.titleCharacterization of ligand binding to Dopamine D3 receptor using fluorescence anisotropy and radioligand bindinget
dc.typeThesiset

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