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- W2012213517 abstract "There exists some confusion over the classification of drugs as either uptake inhibitors or releasing agents for biogenic amines. We have evaluated this problem with rat brain tissue slices (neostriatum and cortex), using [3H]dopamine and the following compounds: potassium chloride, tyramine, d-and l-amphetamine, cocaine, amantacline, desipramine. amitriptyline, nortriptyline and protriptyline. Additional experiments were performed with l-dopa and [3H]serotonin in slices from whole rat brain. Potassium chloride and tyramine. both strong releasing agents, diminished the accumulation of [3H]dopamine during uptake studies. l-Dopa also caused release of [3H]serotonin and an inhibition of [3H]serotonin accumulation. Whenever a releasing action was observed, there was always a diminution in the amount of [3H]amine accumulation and this action (expressed as a per cent effect) was at least equal in magnitude to the per cent released. On the other hand, cocaine was an example of a pure uptake inhibitor; it did not evoke a releasing action at concentrations where a powerful uptake inhibition was seen. From these data, it was possible to conclude that, in the tissue slice system, an experimentally observed release was real (that is. not materially affected by blockade of reuptake), whereas a releasing action evoked an apparent inhibition of uptake equal in magnitude to the releasing action. Before a drug can be designated as an uptake inhibitor, the dose-response curve for inhibition of [3H]amine accumulation should be distinctly to the left of the dose-response curve for release. Our data indicate that, in the neostriatum, all of the drugs studied except cocaine were pure releasing agents and that drugs previously designated as uptake inhibitors were releasing agents. In the cortex, strong inhibition of uptake without significant releasing action was evident for many of the drugs." @default.
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- W2012213517 date "1975-04-01" @default.
- W2012213517 modified "2023-10-11" @default.
- W2012213517 title "Studies on the distinction between uptake inhibition and release of [3H]dopamine in rat brain tissue slices" @default.
- W2012213517 cites W1971230562 @default.
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- W2012213517 doi "https://doi.org/10.1016/0006-2952(75)90152-5" @default.
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