title: Brain receptors for antipsychotic drugs and dopamine: direct binding assays.
abstract: In order to test the suggestion that antipsychotic drugs act by blocking dopamine receptors in the brain, the direct effects of such neuroleptic drugs were tested on the stereospecific binding of [3H]dopamine and of [3H]haloperidol to rat brain striata and their subfractions. The stereospecific component of binding was defined as that amount of [3h]dopamine or [3H]haloperidol bound in the presence of (-)-butaclamol (an inactive drug) minus that bound in the presence of (+)-butaclamol (a potent neuroleptic drug); 100 nM butaclamol was used for the [3H]haloperidol assay, while 1 muM butaclamol was used for the [3H]dopamine assay. Various antipsychotic drugs inhibited this stereospecific component in both the dopamine and haloperidol assays. These inhibitory potencies correlated with the clinical doses used for controlling schizophrenia.
mesh_terms: D000818:Animals; D001665:Binding Sites; D003342:Corpus Striatum / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism*; D006220:Haloperidol / Q000378:metabolism*; D006801:Humans; D008297:Male; D051381:Rats; D011955:Receptors, Drug; D012559:Schizophrenia / Q000188:drug therapy; D013574:Synaptosomes / Q000378:metabolism; D014149:Tranquilizing Agents / Q000378:metabolism* / Q000627:therapeutic use
chemical_list: D011955:Receptors, Drug; D014149:Tranquilizing Agents; D006220:Haloperidol; D004298:Dopamine