Comparison of Dopamine D3 and D2 Receptor Occupancies by a Single Dose of Blonanserin in Healthy Subjects: A Positron Emission Tomography Study With [11C]-(+)-PHNO

The International Journal of Neuropsychopharmacology
Amane TatenoYoshiro Okubo

Abstract

Blockade of D3 receptor, a member of the dopamine D2-like receptor family, has been suggested as a possible medication for schizophrenia. Blonanserin has high affinity in vitro for D3 as well as D2 receptors. We investigated whether a single dose of 12 mg blonanserin, which was within the daily clinical dose range (i.e., 8-24 mg) for the treatment of schizophrenia, occupies D3 as well as D2 receptors in healthy subjects. Six healthy males (mean 35.7±7.6 years) received 2 positron emission tomography scans, the first prior to taking blonanserin, and the second 2 hours after the administration of a single dose of 12 mg blonanserin. Dopamine receptor occupancies by blonanserin were evaluated by [11C]-(+)-PHNO. Occupancy of each region by 12 mg blonanserin was: caudate (range 64.3%-81.5%; mean±SD, 74.3±5.6%), putamen (range 60.4%-84.3%; mean±SD, 73.3%±8.2%), ventral striatum (range 40.1%-88.2%; mean±SD, 60.8%±17.1%), globus pallidus (range 65.8%-87.6%; mean±SD, 75.7%±8.6%), and substantia nigra (range 56.0%-88.7%; mean±SD, 72.4%±11.0%). Correlation analysis between plasma concentration of blonanserin and receptor occupancy in D2-rich (caudate and putamen) and D3-rich (globus pallidus and substantia nigra) regions showed that EC50 f...Continue Reading

References

Nov 1, 1991·The American Journal of Psychiatry·K L DavisM Davidson
Dec 24, 2005·Biological Psychiatry·Matthäus WilleitAlan A Wilson
Apr 25, 2006·Journal of Clinical Psychopharmacology·Akihiro TakanoKazutoshi Suzuki
Oct 13, 2006·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Nathalie GinovartAlan A Wilson
May 24, 2007·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Robert B InnisRichard E Carson
Sep 16, 2009·The International Journal of Neuropsychopharmacology·Ariel Graff-GuerreroShitij Kapur
Apr 23, 2010·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Patrick N McCormickAlan A Wilson
May 22, 2010·European Journal of Clinical Pharmacology·Junji SaruwatariSunao Kaneko
Dec 24, 2010·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Ragy R GirgisMark Slifstein
Jun 11, 2011·European Journal of Pharmacology·Yoshihiro TadoriTetsuro Kikuchi
Jan 27, 2012·Human Psychopharmacology·Tomomi TenjinNoboru Yamaguchi
Oct 3, 2012·Handbook of Experimental Pharmacology·Gerhard Gross, Karla U Drescher
Nov 7, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Gerhard GrossKarla U Drescher
Jun 25, 2013·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Shinichiro NakajimaAriel Graff-Guerrero
Aug 15, 2014·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Hirotake HidaYukihiro Noda
Apr 4, 2015·Journal of Pharmacological Sciences·Satoko BabaMichiko Ono

Related Concepts

11C-PHNO
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