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- W2040803902 abstract "The accumulation of 3H-labelled dopamine ([3H]DA) in crude synaptosomal fractions from rat corpus striatum was found to be time and temperature dependent. The accumulation was saturable with a Km value of 105 nM and was inhibited noncompetitively by benztropine. Series of thymoleptics, neuroleptics, stimulants, and miscellaneous compounds were tested for inhibiting properties in the system. The concentration-response curves were parallel to that of benztropine. The thymoleptics were rather weak inhibitors with potencies not comparable to their inhibition of either noradrenaline or serotonin uptake. Only a few neuroleptics (diphenylbutylpiperidines) showed potencies comparable to benztropine, whereas most of the neuroleptics were rather weak. The isomers of the thioxanthenes were almost equipotent, and the potencies of the neuroleptics claimed to induce few extrapyramidal side effects varied considerably but covered the same concentrations as the neuroleptics normally inducing these side effects. The stimulants were all rather potent, whereas anti-cholinergics were very weak and GABA uptake inhibitors were without effect. It is concluded, that the accumulation of [3H]DA clearly deviates in steric requirements from the uptake of noradrenaline, serotonin and γ-aminobutyric acid, and probably represents the difference between DA uptake and release. Furthermore, the test does not seem to be predictive for clinical effects of antidepressants and neuroleptics." @default.
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- W2040803902 title "Inhibition of [3H]dopamine accumulation in rat striatal synaptosomes by psychotropic drugs" @default.
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- W2040803902 doi "https://doi.org/10.1016/0006-2952(78)90159-4" @default.
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