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Effects of Aripiprazole, Risperidone, and Olanzapine on 5-HT1A Receptors in Patients With Schizophrenia

Lerond, Jérôme MD*; Lothe, Amélie PhD*†‡§∥¶; Ryvlin, Philippe MD, PhD†‡§∥¶#; Bouvard, Sandrine PhD†‡§∥¶; d’Amato, Thierry MD, PhD†‡**††; Ciumas, Carolina PhD†‡§∥¶; Daléry, Jean MD*†‡**; Poulet, Emmanuel MD, PhD**††; Saoud, Mohamed MD, PhD*†‡**

Journal of Clinical Psychopharmacology: February 2013 - Volume 33 - Issue 1 - p 84–89
doi: 10.1097/JCP.0b013e31827b97a6
Brief Reports

Abstract: To investigate the impact of various antipsychotic drugs on the 5-HT1A serotoninergic system, we performed a [18F]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 [18F]MPPF-binding potential (BPND). A significant reduction of [18F]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 [18F]MPPF BPND compared with healthy subjects and schizophrenic patients with SGA treatment. In addition, compared with matched controls, the reduction of regional [18F]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.

From the *Department Consultation-Liaison Psychiatry, Hospices Civils deLyon; †Université de Lyon, Lyon; ‡Université Lyon 1, Villeurbanne; §Institute for Children and Adolescents with Epilepsy (IDEE); ∥INSERM, U1028, Lyon Neuroscience Research Center, Tiger Team; ¶CNRS, UMR5292, Lyon Neuroscience Research Center, Tiger Team, Lyon; #Department of Functional Neurology and Epileptology, Hospices Civils de Lyon; **EAM 4166, Lyon; ††CH Le Vinatier, Bron, France.

Received April 19, 2011; accepted after revision May 8, 2012.

Reprints: Amélie Lothe, PhD, CERMEP, 59 Bd Pinel, 69003, Lyon, France (e-mail:

This study was partly funded by an unrestricted grant from Scientific Research Committee of Le Vinatier Hospital.

J Lerond and A Lothe are co-first authors.

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© 2013 Lippincott Williams & Wilkins, Inc.