Dopamine Receptor Binding Predicts Clinical and Pharmacological Potencies of Antischizophrenic Drugs

J Neuropsychiatry Clin Neurosci. Spring 1996;8(2):223-6. doi: 10.1176/jnp.8.2.223.

Abstract

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.

MeSH terms

  • Antipsychotic Agents / pharmacokinetics*
  • Antipsychotic Agents / therapeutic use*
  • Binding Sites*
  • Butyrophenones / pharmacokinetics*
  • Butyrophenones / therapeutic use*
  • Corpus Striatum / metabolism
  • Humans
  • Nucleus Accumbens / metabolism
  • Phenothiazines / pharmacokinetics*
  • Phenothiazines / therapeutic use*
  • Receptors, Dopamine / metabolism*
  • Schizophrenia / drug therapy*

Substances

  • Antipsychotic Agents
  • Butyrophenones
  • Phenothiazines
  • Receptors, Dopamine