Measurement of the serotonin 1A receptor availability in patients with schizophrenia during treatment with the antipsychotic medication ziprasidone

J Psychopharmacol. 2011 Jun;25(6):734-43. doi: 10.1177/0269881110388329. Epub 2010 Nov 25.


The aim of this study was to compare 5-HT(1A) availability in vivo in individuals with schizophrenia before and during treatment with the atypical antipsychotic ziprasidone. Six individuals with schizophrenia underwent two PET scans with [(11)C]WAY 100635; the first while medication-free (baseline) and the second while taking the atypical antipsychotic ziprasidone (on-medication). Regional volumes of distribution (V(T), mL g(-1)) were derived using a two-tissue compartment kinetic model. Outcome measures included binding potential relative to the plasma (BP(P), mL g(-1)) and the binding potential relative to the nonspecific distribution volume (BP(ND), unitless). No significant differences were observed in regional BP(P) or BP(ND) with ziprasidone treatment. A significant correlation was noted between BP(P) measured in the orbitofrontal cortex during the on-medication condition and degree of improvement in negative symptoms with treatment (r = 0.96, p = 0.004). Consistent with the published literature of changes in 5-HT(1A) binding during treatment with 5-HT(1A) receptor agonists, this study did not detect a significant reduction in 5-HT(1A) binding with ziprasidone. The finding of a relationship between 5-HT(1A) binding and the degree of improvement in negative symptoms provides further support for the role of the 5-HT(1A) receptor in the pathophysiology and treatment of this symptom domain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antipsychotic Agents / pharmacology
  • Antipsychotic Agents / therapeutic use
  • Brain / drug effects
  • Brain / metabolism*
  • Carbon Radioisotopes
  • Female
  • Humans
  • Magnetic Resonance Imaging / methods
  • Male
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use*
  • Positron-Emission Tomography / methods
  • Psychiatric Status Rating Scales
  • Pyridines
  • Radioligand Assay / methods
  • Receptor, Serotonin, 5-HT1A / metabolism*
  • Schizophrenia / diagnosis
  • Schizophrenia / drug therapy*
  • Schizophrenia / metabolism*
  • Serotonin Antagonists
  • Thiazoles / pharmacology*
  • Thiazoles / therapeutic use*


  • Antipsychotic Agents
  • Carbon Radioisotopes
  • Piperazines
  • Pyridines
  • Serotonin Antagonists
  • Thiazoles
  • Receptor, Serotonin, 5-HT1A
  • ziprasidone
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide