Article: article from journal or magazin.
The time course of binding to striatal dopamine D2 receptors by the neuroleptic ziprasidone (CP-88,059-01) determined by positron emission tomography.
Publication types: Clinical Trial ; Comparative Study ; Controlled Clinical Trial ; Journal Article ; Research Support, Non-U.S. Gov'tPublication Status: ppublish
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.
Adult, Antipsychotic Agents/metabolism, Antipsychotic Agents/pharmacokinetics, Corpus Striatum/metabolism, Corpus Striatum/radionuclide imaging, Humans, Male, Piperazines/metabolism, Piperazines/pharmacokinetics, Prolactin/blood, Raclopride, Receptors, Dopamine D2/metabolism, Salicylamides/diagnostic use, Thiazoles/metabolism, Thiazoles/pharmacokinetics, Time Factors, Tomography, Emission-Computed
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