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- W2089035381 abstract "Adenosine is a nucleoside displaying various biological effects via stimulation of four G-protein–coupled receptors, A1, A2A, A2B, and A3. Adenosine also modulates voltage-gated (Kv) and small conductance calcium-activated (SKCa) potassium channels. The effect of these potassium channels on the expression of adenosine receptors is poorly understood. We evaluated the action of BgK (a natural Kv channel blocker) and Lei-Dab7 (a synthetic SKCa channel blocker) on the expression of adenosine A2A receptors (A2AR) in Jurkat human T cells. We found that Lei-Dab7, but not BgK, increased the maximal binding value of the tritiated ligand ZM241385 to A2AR in a dose-dependent manner (+45% at 5 nM; +70% at 50 nM as compared to control). These results were further confirmed by Western blotting using a specific monoclonal antibody to human A2AR. The ligand affinity-related dissociation constant and A2AR mRNA amount were not significantly modified by either drug. We suggest that modulation of SKCa channels can influence membrane expression of A2AR and thus has a therapeutic potential." @default.
- W2089035381 created "2016-06-24" @default.
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- W2089035381 date "2013-04-01" @default.
- W2089035381 modified "2023-09-26" @default.
- W2089035381 title "SKCa Channels Blockage Increases the Expression of Adenosine A2AReceptor in Jurkat Human T Cells" @default.
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- W2089035381 doi "https://doi.org/10.1089/biores.2012.0282" @default.
- W2089035381 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3620471" @default.
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- W2089035381 hasPublicationYear "2013" @default.
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