Striatal and extrastriatal dopamine D2 receptor occupancy by a novel antipsychotic, blonanserin: a PET study with [11C]raclopride and [11C]FLB 457 in schizophrenia

Journal of Clinical Psychopharmacology
Amane TatenoYoshiro Okubo

Abstract

Blonanserin is a novel antipsychotic with high affinities for dopamine D(2) and 5-HT(2A) receptors, and it was recently approved for the treatment of schizophrenia in Japan and Korea. Although double-blind clinical trials have demonstrated that blonanserin has equal efficacy to risperidone, and with a better profile especially with respect to prolactin elevation, its profile of in vivo receptor binding has not been investigated in patients with schizophrenia. Using positron emission tomography (PET), we measured striatal and extrastriatal dopamine D(2) receptor occupancy by blonanserin in 15 patients with schizophrenia treated with fixed doses of blonanserin (ie, 8, 16, and 24 mg/d) for at least 4 weeks before PET scans, and in 15 healthy volunteers. Two PET scans, 1 with [(11)C]raclopride for the striatum and 1 with [(11)C]FLB 457 for the temporal cortex and pituitary, were performed on the same day. Striatal dopamine D(2) receptor occupancy by blonanserin was 60.8% (3.0%) [mean (SD)] at 8 mg, 73.4% (4.9%) at 16 mg, and 79.7% (2.3%) at 24 mg. The brain/plasma concentration ratio calculated from D(2) receptor occupancy in the temporal cortex and pituitary was 3.38, indicating good blood-brain barrier permeability. This was the ...Continue Reading

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Apr 3, 2013·European Journal of Clinical Pharmacology·Melvin GeorgeSteven Aibor Dkhar
Jan 24, 2014·The International Journal of Neuropsychopharmacology·WooChan KimYoshiro Okubo
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Jun 28, 2017·Brain Research·Kerstin HeurlingMark Lubberink
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May 29, 2020·Neuropsychopharmacology Reports·Ryosuke ArakawaC Halldin

Related Concepts

FLB 457, hydrobromide, (S)-isomer
Lonasen
Blood - Brain Barrier Anatomy
Brain
Lentiform Nucleus Structure
Dose-Response Relationship, Drug
Piperazines
Piperidines
Pyrrolidines
Salicylamides

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