Chronic clozapine treatment down-regulates serotonin 5-HT-1c receptors in rat brain

Prog Neuropsychopharmacol Biol Psychiatry. 1992 Sep;16(5):727-32. doi: 10.1016/0278-5846(92)90028-d.

Abstract

1. The effects of chronic treatment with the atypical antipsychotic, clozapine, and classical antipsychotic, haloperidol, on serotonergic 5-HT-1c and dopamine D2 receptors in rat brain were studied with radioligand binding methods. 2. Two weeks' treatment with clozapine did not alter striatal D2 receptor characteristics measured with 3H-spiperone, but caused a 54% down-regulation of 3H-mesulergine binding to 5-HT-1c receptors in choroid plexus. 3. In contrast, two weeks' treatment with a classical neuroleptic, haloperidol increased significantly D2 receptor number in striatum, but had no effect on 5-HT-1c receptor binding. 4. In conclusion, alterations of 5-HT-1c receptor characteristics after chronic clozapine treatment may represent a mechanism that contributes to the unique clinical profile of this antipsychotic drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / drug effects*
  • Clozapine / pharmacology*
  • Down-Regulation / drug effects*
  • Haloperidol / pharmacology
  • Male
  • Radioligand Assay
  • Rats
  • Rats, Inbred Strains
  • Receptors, Serotonin / drug effects*

Substances

  • Receptors, Serotonin
  • Clozapine
  • Haloperidol