Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs.
Tritiated haloperidol and tritiated dopamine label postsynaptic dopamine receptors in mammalian brain. Clinical potencies of butyrophenones, phenothiazines, and related drugs correlate closely with their ability to inhibit tritiated haloperidol binding. These binding methods provide a simple in vitro means for evaluating new drugs as potential antischizophrenic agents.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism* / Q000627:therapeutic use; D001667:Binding, Competitive; D002090:Butyrophenones / Q000378:metabolism* / Q000627:therapeutic use; D003342:Corpus Striatum / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism; D018492:Dopamine Antagonists; D006220:Haloperidol / Q000378:metabolism; D006801:Humans; D009830:Olfactory Bulb / Q000378:metabolism; D010640:Phenothiazines; D011955:Receptors, Drug; D012559:Schizophrenia / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D002090:Butyrophenones; D018492:Dopamine Antagonists; D010640:Phenothiazines; D011955:Receptors, Drug; D000262:Adenylyl Cyclases; D006220:Haloperidol; D004298:Dopamine