Brain region binding of the D2/3 agonist [11C]-(+)-PHNO and the D2/3 antagonist [11C]raclopride in healthy humans

Human Brain Mapping
Ariel Graff-GuerreroShitij Kapur

Abstract

The D(2) receptors exist in either the high- or low-affinity state with respect to agonists, and while agonists bind preferentially to the high-affinity state, antagonists do not distinguish between the two states. [(11)C]-(+)-PHNO is a PET D(2) agonist radioligand and therefore provides a preferential measure of the D(2) (high) receptors. In contrast, [(11)C]raclopride is an antagonist radioligand and thus binds with equal affinity to the D(2) high- and low-affinity states. The aim was to compare the brain uptake, distribution and binding characteristics between [(11)C]-(+)-PHNO and [(11)C]raclopride in volunteers using a within-subject design. Both radioligands accumulated in brain areas rich in D(2)/D(3)-receptors. However, [(11)C]-(+)-PHNO showed preferential uptake in the ventral striatum and globus pallidus, while [(11)C]raclopride showed preferential uptake in the dorsal striatum. Mean binding potentials were higher in the putamen (4.3 vs. 2.8) and caudate (3.4 vs 2.1) for [(11)C]raclopride, equal in the ventral-striatum (3.4 vs. 3.3), and higher in the globus pallidus for [(11)C]-(+)-PHNO (1.8 vs. 3.3). Moreover [(11)C]-(+)-PHNO kinetics in the globus pallidus showed a slower washout than other regions. One explanation ...Continue Reading

References

Nov 7, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Gerhard GrossKarla U Drescher
Dec 12, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Jan-Peter van WieringenMartin C Michel
Feb 19, 2013·Psychopharmacology·Takefumi SuzukiDavid C Mamo
Nov 7, 2008·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Ariel Graff-GuerreroShitij Kapur
Apr 22, 2011·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Camilo de la Fuente-SandovalAriel Graff-Guerrero
Aug 8, 2013·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Doris PayerIsabelle Boileau
Jan 21, 2009·Brain : a Journal of Neurology·Isabelle BoileauStephen J Kish
Jan 27, 2012·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Isabelle BoileauStephen J Kish
May 31, 2014·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Fernando CaravaggioAriel Graff-Guerrero
Sep 4, 2013·Progress in Neuro-psychopharmacology & Biological Psychiatry·Doris PayerIsabelle Boileau
Jan 4, 2013·Expert Opinion on Therapeutic Patents·Fabrizio Micheli, Christian A Heidbreder
Mar 6, 2016·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Fernando CaravaggioAriel Graff-Guerrero
Aug 5, 2008·Methods : a Companion to Methods in Enzymology·Henning BoeckerThomas R Tölle
Feb 21, 2008·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Lisa A BriandTerry E Robinson
Jun 11, 2015·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Shinichiro NakajimaAriel Graff-Guerrero
Sep 18, 2007·Biological Psychology·Rachel TomerNora D Volkow
Dec 15, 2010·CNS Neuroscience & Therapeutics·Magdalena Nord, Lars Farde
Mar 6, 2010·Annals of the New York Academy of Sciences·Christian A Heidbreder, Amy H Newman
Apr 2, 2013·Biological Psychiatry·Fernando CaravaggioAriel Graff-Guerrero
Mar 17, 2015·Movement Disorders : Official Journal of the Movement Disorder Society·Léon TremblayJean Féger
Mar 15, 2014·Journal of Neurology·Flavia NiccoliniMarios Politis
Mar 31, 2015·Clinica Chimica Acta; International Journal of Clinical Chemistry·Fernando CaravaggioAriel Graff-Guerrero
Jan 8, 2015·Bioorganic & Medicinal Chemistry·Amelie L BartuschatMarkus R Heinrich
Feb 27, 2015·The International Journal of Neuropsychopharmacology·Fernando CaravaggioAriel Graff-Guerrero
Jan 15, 2014·Neuron·Lissandra Castellan BaldanChristopher Pittenger
Apr 11, 2014·Drug and Alcohol Dependence·David MatuskeyYu-Shin Ding

Citations

Aug 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·S FerreK Fuxe
Sep 1, 1988·Journal of Neurochemistry·B K MadrasR D Spealman
Aug 31, 1988·Neuroscience Letters·J De KeyserG Vauquelin
Mar 1, 1995·Trends in Pharmacological Sciences·P Leff
May 1, 1995·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·K J Friston
Aug 1, 1993·Synapse·Philip SeemanP S Anderson
Nov 8, 1994·Proceedings of the National Academy of Sciences of the United States of America·A M MurrayJ N Joyce
Jul 1, 1994·Synapse·Jose Nobrega, Philip Seeman
Jan 1, 1993·International Review of Neurobiology·David R SibleyY Shen
Jan 1, 1996·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·A A LammertsmaR S Frackowiak
Feb 1, 1996·Alcoholism, Clinical and Experimental Research·N F Tajuddin, M J Druse
Dec 1, 1996·NeuroImage·A A Lammertsma, S P Hume
Feb 11, 1998·Physiological Reviews·C MissaleM G Caron
Jan 14, 1999·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·E V Gurevich, J N Joyce
Feb 3, 1999·Annals of the New York Academy of Sciences·C Scaramellini, P Leff
Jan 14, 2000·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Wayne DrevetsChester A Mathis
Nov 1, 2000·Nuclear Medicine and Biology·Alan A WilsonSylvain Houle
Feb 13, 2001·Biological Psychiatry·Wayne DrevetsChester A Mathis
Aug 29, 2001·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Osama MawlawiMarc A Laruelle
Mar 22, 2002·NeuroImage·Christopher R GenoveseThomas Nichols
Jun 13, 2002·Neuroreport·Françoise KoShitij Kapur
Mar 7, 2003·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Diana MartinezMarc A Laruelle
Feb 18, 2005·Proceedings of the National Academy of Sciences of the United States of America·Philip SeemanTeresa Tallerico
Dec 24, 2005·Biological Psychiatry·Matthäus WilleitAlan A Wilson
Jun 2, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Robert M KesslerHerbert Y Meltzer
Jun 21, 2006·Synapse·Philip SeemanTomiki Sumiyoshi
Jun 27, 2006·Psychiatry Research·Pablo M RusjanShitij Kapur

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