title: Effects of aripiprazole, risperidone, and olanzapine on 5-HT1A receptors in patients with schizophrenia.
abstract: To investigate the impact of various antipsychotic drugs on the 5-HT1A serotoninergic system, we performed a [F]4-(2-methoxyphenyl)-1-[2-(N-2-pirydynyl)-p-luorobenzamido]-ethyl-piperazine PET study in 19 schizophrenic patients treated with either aripiprazole, which has a partial agonist activity at 5-HT1A receptors, or second-generation antipsychotics (SGA) (olanzapine or risperidone), which do not demonstrate such property. We used a simplified reference tissue model to generate parametric images of [F]MPPF-binding potential (BPND). A significant reduction of [F]MPPF BPND was found in treated schizophrenic patients compared to age- and sex-matched healthy subjects. These modifications were mainly localized in the frontal and orbitofrontal cortex and may reflect either the pathophysiology of schizophrenia or medication effects. The schizophrenic patients treated with aripiprazole showed a reduction of global [F]MPPF BPND compared with healthy subjects and schizophrenic patients with SGA treatment. In addition, compared with matched controls, the reduction of regional [F]MPPF BPND was more marked in the schizophrenic patients treated with aripiprazole compared with those receiving SGA treatment, possibly reflecting the partial agonist of aripiprazole activity at 5-HT1A receptors.
authors.affiliation: Department Consultation-Liaison Psychiatry, Hospices Civils deLyon, France.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Lerond
authors.forename: Amélie
authors.initials: A
authors.lastname: Lothe
authors.forename: Philippe
authors.initials: P
authors.lastname: Ryvlin
authors.forename: Sandrine
authors.initials: S
authors.lastname: Bouvard
authors.forename: Thierry
authors.initials: T
authors.lastname: d'Amato
authors.forename: Carolina
authors.initials: C
authors.lastname: Ciumas
authors.forename: Jean
authors.initials: J
authors.lastname: Daléry
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Poulet
authors.forename: Mohamed
authors.initials: M
authors.lastname: Saoud
mesh_terms: D000328:Adult; D000704:Analysis of Variance; D014150:Antipsychotic Agents / Q000627:therapeutic use*; D000068180:Aripiprazole; D001569:Benzodiazepines / Q000378:metabolism / Q000627:therapeutic use*; D016022:Case-Control Studies; D002540:Cerebral Cortex / Q000000981:diagnostic imaging / Q000187:drug effects* / Q000378:metabolism; D054333:Drug Partial Agonism; D005260:Female; D006801:Humans; D008279:Magnetic Resonance Imaging; D008297:Male; D000077152:Olanzapine; D010879:Piperazines / Q000378:metabolism / Q000627:therapeutic use*; D049268:Positron-Emission Tomography; D011725:Pyridines; D015363:Quinolones / Q000378:metabolism / Q000627:therapeutic use*; D019275:Radiopharmaceuticals; D044282:Receptor, Serotonin, 5-HT1A / Q000187:drug effects* / Q000378:metabolism; D018967:Risperidone / Q000378:metabolism / Q000627:therapeutic use*; D012559:Schizophrenia / Q000175:diagnosis / Q000000981:diagnostic imaging / Q000188:drug therapy* / Q000378:metabolism; D012565:Schizophrenic Psychology; D016896:Treatment Outcome; D055815:Young Adult
chemical_list: D014150:Antipsychotic Agents; D010879:Piperazines; D011725:Pyridines; D015363:Quinolones; D019275:Radiopharmaceuticals; D044282:Receptor, Serotonin, 5-HT1A; D001569:Benzodiazepines; D000068180:Aripiprazole; D018967:Risperidone; C416325:4-(2'-methoxyphenyl)-1-(2'-(N-2'-pyridinyl)-p-(18F)fluorobenzamido )ethylpiperazine; D000077152:Olanzapine