Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: clozapine potently interacts with 5-HT1C sites

Eur J Pharmacol. 1990 Nov 20;191(1):93-6. doi: 10.1016/0014-2999(90)94100-c.

Abstract

We determined the affinity of several typical and atypical antipsychotics for the 5-HT1C and 5-HT2 sites using radioligand binding assays. Most of the antipsychotics tested appeared to bind to 5-HT2 sites with affinities that were fairly high (i.e. pKi values between 7 and 9) and significantly higher than for 5-HT1C sites. In contrast, clozapine was found to have a significantly higher affinity for 5-HT1C than for 5-HT2 sites. Clozapine had the highest affinity for 5-HT1C sites of all the compounds tested. These findings are consistent with the hypothesis that an interaction with 5-HT2 receptors may be relevant to the clinical activity of typical antipsychotics. The findings also suggest, however, that an interaction with 5-HT1C sites may be relevant to the mechanism of clinical action of clozapine and, perhaps, of other atypical antipsychotics.

MeSH terms

  • Animals
  • Antipsychotic Agents / metabolism*
  • Binding Sites
  • Choroid Plexus / metabolism
  • Clozapine / metabolism*
  • Ergolines / metabolism
  • In Vitro Techniques
  • Ketanserin / metabolism
  • Kinetics
  • Receptors, Serotonin / classification
  • Receptors, Serotonin / metabolism*
  • Swine

Substances

  • Antipsychotic Agents
  • Ergolines
  • Receptors, Serotonin
  • Ketanserin
  • Clozapine
  • mesulergine