The time course of binding to striatal dopamine D2 receptors by the neuroleptic ziprasidone (CP-88,059-01) determined by positron emission tomography.
Détails
ID Serval
serval:BIB_B94C483F6EDF
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
The time course of binding to striatal dopamine D2 receptors by the neuroleptic ziprasidone (CP-88,059-01) determined by positron emission tomography.
Périodique
Psychopharmacology
ISSN
0033-3158 (Print)
ISSN-L
0033-3158
Statut éditorial
Publié
Date de publication
1996
Volume
124
Numéro
1-2
Pages
141-147
Langue
anglais
Notes
Publication types: Clinical Trial ; Comparative Study ; Controlled Clinical Trial ; Journal Article ; Research Support, Non-U.S. Gov'tPublication Status: ppublish
Résumé
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.
Mots-clé
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
Pubmed
Web of science
Création de la notice
16/09/2011 18:55
Dernière modification de la notice
20/08/2019 15:27