The time course of binding to striatal dopamine D2 receptors by the neuroleptic ziprasidone (CP-88,059-01) determined by positron emission tomography

Psychopharmacology (Berl). 1996 Mar;124(1-2):141-7. doi: 10.1007/BF02245614.


Positron emission tomography (PET) and 11C-raclopride were used to assess the time course of binding to central dopamine D2 receptors by the novel neuroleptic ziprasidone. In a third party blind study, six healthy male control subjects received a predose of 40 mg ziprasidone and were scanned at an interval of between 4 and 36 h post-dose. One additional subject was assigned to placebo predose and was scanned at 4 h post-dose. Binding potential (BP) was compared with that seen in the subject predosed with placebo and with that seen in nine unmedicated normal volunteers. Subjects studied up to 12 h post-dose had BPs that were greater than 2 SD less than the mean BP, indicative of extensive D2 receptor binding by ziprasidone. With increasing time between dosing and PET scanning there was a curvilinear increase in BP, so that all studies performed at or after 18 h post-dose gave BPs in the normal range (mean +/- 2 SD). Elevated prolactin levels returned to within the normal range by 18 h post-dose. PET measures of binding potential correlated significantly with serum levels of ziprasidone at the time of scanning and less significantly with absolute prolactin levels at the same time.

Publication types

  • Clinical Trial
  • Comparative Study
  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antipsychotic Agents / metabolism*
  • Antipsychotic Agents / pharmacokinetics
  • Corpus Striatum / diagnostic imaging
  • Corpus Striatum / metabolism*
  • Humans
  • Male
  • Piperazines / metabolism*
  • Piperazines / pharmacokinetics
  • Prolactin / blood
  • Raclopride
  • Receptors, Dopamine D2 / metabolism*
  • Salicylamides
  • Thiazoles / metabolism*
  • Thiazoles / pharmacokinetics
  • Time Factors
  • Tomography, Emission-Computed


  • Antipsychotic Agents
  • Piperazines
  • Receptors, Dopamine D2
  • Salicylamides
  • Thiazoles
  • Raclopride
  • ziprasidone
  • Prolactin