Tefludazine is an orally active antagonist of dopamine D 2 receptor with an IC 50 of 8.8 nM and 5-HT 2 receptor with an IC 50 of 8.6 nM. Tefludazine moderately inhibits the uptake of dopamine, norepinephrine and serotonin in rat brain synaptosomes, with IC 50 values of 520 nM, 660 nM and 7000 nM, respectively . Tefludazine exhibits long-acting antipsychotic activity, lacks anticholinergic activity, shows Clozapine ( HY-14539 )-like effects at low doses and Haloperidol ( HY-14538 )-like effects at high doses. Tefludazine can be used for the research of psychotic disorders.
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