D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: a PET study in a receptor internalization-deficient mouse model

Skinbjerg, Mette; Liow, Jeih-San; Seneca, Nicholas; Hong, Jinsoo; Lu, Shuiyu; Thorsell, Annika; Heilig, Markus; Pike, Victor W.; Halldin, Christer; Sibley, David R.; Innis, Robert B.

doi:10.1016/j.neuroimage.2010.01.055

Cited by 86Neurotransmitter Receptor Influence on BehaviorReceptor Mechanisms and SignalingNeuroscience and Neuropharmacology Research

D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: a PET study in a receptor internalization-deficient mouse model

Open access

Skinbjerg, Mette, Liow, Jeih-San, Seneca, Nicholas, Hong, Jinsoo, Lu, Shuiyu, Thorsell, Annika, Heilig, Markus, Pike, Victor W. +3 more·2010·NeuroImage

DOI 10.1016/j.neuroimage.2010.01.055PMC PMC2838946

Open this paper in CoChat — free account

Abstract

Dopamine released by amphetamine decreases the in vivo binding of PET radioligands to the dopamine D(2) receptor. Although concentrations of extracellular dopamine largely return to baseline within 1 to 2 h after amphetamine treatment, radioligand binding remains decreased for several hours. The purpose of this study was to determine whether the prolonged decrease of radioligand binding after amphetamine administration is caused by receptor internalization. To distinguish dopamine displacement from receptor internalization, we used wild-type and arrestin3 (arr3) knockout mice, which are incapable of internalizing D(2) receptors. In addition, we used both the D(2) selective agonist [(11)C]MNPA (which is thought to bind to the high affinity state of the receptor) and the D(2) selective antagonist [(18)F]fallypride (which does not differentiate between high and low affinity state). After an initial baseline scan, animals were divided in three groups for a second scan: either 30 min or 4 h after amphetamine administration (3 mg/kg, i.p.) or as retest. At 30 min, [(11)C]MNPA showed greater displacement than [(18)F]fallypride, but each radioligand gave similar displacement in knockout and wild-type mice. At 4 h, the binding of both radioligands returned to baseline in arr3 knockout mice, but remained decreased in wild-type mice. Radioligand binding was unaltered on retest scanning. Our results suggest that the prolonged decrease of radioligand binding after amphetamine is mainly due to internalization of the D(2) receptor rather than dopamine displacement. In addition, this study demonstrates the utility of small animal PET to study receptor trafficking in vivo in genetically modified mice.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1016/j.neuroimage.2010.01.055

Cites

34 of 34 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

The Mouse Brain in Stereotaxic Coordinates
Paxinos, G. (2001) · Cited by 12,859 · see citing works
Consensus Nomenclature for in vivo Imaging of Reversibly Binding Radioligands
Innis, R. B., Cunningham, V. J., Delforge, J., Fujita, M., Gjedde, A., Gunn, R. N., Holden, J., Houle, S., Huang, S.-C., Ichise, M., et al. (2007) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/sj.jcbfm.9600493 · Cited by 1,955 · see citing works
Self-citation
Transduction of Receptor Signals by ß-Arrestins
Lefkowitz, R. J., & Shenoy, S. K. (2005) · Science · doi:10.1126/science.1109237 · Cited by 1,729 · see citing works
Imaging Synaptic Neurotransmission with in Vivo Binding Competition Techniques: A Critical Review
Laruelle, M. (2000) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1097/00004647-200003000-00001 · Cited by 944 · see citing works
Linearized Reference Tissue Parametric Imaging Methods: Application to [ 11 C]DASB Positron Emission Tomography Studies of the Serotonin Transporter in Human Brain
Ichise, M., Liow, J., Lu, J., Takano, A., Modell, K. J., Toyama, H., Suhara, T., Suzuki, K., Innis, R. B., & Carson, R. E. (2003) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1097/01.wcb.0000085441.37552.ca · Cited by 651 · see citing works
Self-citation
Classical and new roles of β-arrestins in the regulation of G-PROTEIN-COUPLED receptors
Pierce, K. L., & Lefkowitz, R. J. (2001) · Nature reviews. Neuroscience · doi:10.1038/35094577 · Cited by 478 · see citing works
β-Arrestin 1 and 2 differentially regulate heptahelical receptor signaling and trafficking
Kohout, T. A., Lin, F., Perry, S. J., Conner, D. A., & Lefkowitz, R. J. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.98.4.1601 · Cited by 367 · see citing works
Radiosynthesis and Evaluation of [11C]-(+)-4-Propyl-3,4,4a,5,6,10b-hexahydro-2H-naphtho[1,2-b][1,4]oxazin-9-ol as a Potential Radiotracer for in Vivo Imaging of the Dopamine D2 High-Affinity State with Positron Emission Tomography
Wilson, A. A., McCormick, P. N., Kapur, S., Willeit, M., García, A., Hussey, D. F., Houle, S., Seeman, P. M., & Ginovart, N. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm050155n · Cited by 227 · see citing works
Fluorinated benzamide neuroleptics—III. Development of (S)-N-[(1-allyl-2-pyrrolidinyl)methyl]-5-(3-[18F]fluoropropyl)-2,3-dimethoxybenzamide as an improved dopamine D-2 receptor tracer
Mukherjee, J., Yang, Z.-Y., Das, M. K., & Brown, T. (1995) · Nuclear Medicine and Biology · doi:10.1016/0969-8051(94)00117-3 · Cited by 219 · see citing works
Performance Measurement of the microPET Focus 120 Scanner
Kim, J. S., Lee, J. S., Im, K. C., Kim, S. J., Kim, S.-Y., Lee, D. S., & Moon, D. H. (2007) · Journal of Nuclear Medicine · doi:10.2967/jnumed.107.040550 · Cited by 180 · see citing works
Resolution uniformity and sensitivity of the NIH ATLAS small animal PET scanner: Comparison to simulated LSO scanners without depth-of-interaction capability
Seidel, J., Vaquero, J. J., & Green, M. V. (2003) · IEEE Transactions on Nuclear Science · doi:10.1109/tns.2003.817282 · Cited by 166 · see citing works
In vivo vulnerability to competition by endogenous dopamine: Comparison of the D2 receptor agonist radiotracer (–)‐N‐[11C]propyl‐norapomorphine ([11C]NPA) with the D2 receptor antagonist radiotracer [11C]‐raclopride
Narendran, R., Hwang, D., Slifstein, M., Talbot, P., Erritzoe, D., Huang, Y., Cooper, T. B., Martinez, D., Kegeles, L. S., Abi-Dargham, A., et al. (2004) · Synapse · doi:10.1002/syn.20013 · Cited by 156 · see citing works
Binding characteristics and sensitivity to endogenous dopamine of [11C]‐(+)‐PHNO, a new agonist radiotracer for imaging the high‐affinity state of D2 receptors in vivo using positron emission tomography
Ginovart, N., Galineau, L., Willeit, M., Mizrahi, R., Bloomfield, P. M., Seeman, P. M., Houle, S., Kapur, S., & Wilson, A. A. (2006) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2006.03840.x · Cited by 146 · see citing works
Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: a comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride
Seneca, N., Finnema, S. J., Farde, L., Gulyás, B., Wikström, H. V., Halldin, C., & Innis, R. B. (2006) · Synapse · doi:10.1002/syn.20238 · Cited by 110 · see citing works
Self-citation
In vivo evidence for dopamine-mediated internalization of D2-receptors after amphetamine: differential findings with [3H]raclopride versus [3H]spiperone
Sun, W., Ginovart, N., Ko, F., Seeman, P., & Kapur, S. (2003) · Molecular Pharmacology · doi:10.1124/mol.63.2.456 · Cited by 99 · see citing works
G Protein-coupled Receptor Kinase-mediated Phosphorylation Regulates Post-endocytic Trafficking of the D2 Dopamine Receptor
Namkung, Y., Dipace, C., Javitch, J. A., & Sibley, D. R. (2009) · Journal of Biological Chemistry · doi:10.1074/jbc.m900388200 · Cited by 97 · see citing works
Self-citation
Impact of D2 receptor internalization on binding affinity of neuroimaging radiotracers
Guo, N., Guo, W., Králíková, M., Jiang, M., Schieren, I., Narendran, R., Slifstein, M., Abi-Dargham, A., Laruelle, M., Javitch, J., et al. (2009) · Neuropsychopharmacology · doi:10.1038/npp.2009.189 · Cited by 88 · see citing works
Synthesis of [18F]Fallypride in a Micro-Reactor: Rapid Optimization and Multiple-Production in Small Doses for Micro-PET Studies
Lu, S., Giamis, A. M., & Pike, V. W. (2009) · Current Radiopharmaceuticals · doi:10.2174/1874471010902010049 · Cited by 85 · see citing works
Self-citation
Specific Binding of [ 11 C]Raclopride and N -[ 3 H]Propyl-Norapomorphine to Dopamine Receptors in Living Mouse Striatum: Occupancy by Endogenous Dopamine and Guanosine Triphosphate–Free G Protein
Cumming, P., Wong, D. F., Gillings, N., Hilton, J., Scheffel, U., & Gjedde, A. (2002) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1097/00004647-200205000-00011 · Cited by 71 · see citing works
Oral <scp>D</scp>‐amphetamine causes prolonged displacement of [11C]raclopride as measured by PET
Cárdenas, L., Houle, S., Kapur, S., & Busto, U. E. (2004) · Synapse · doi:10.1002/syn.10282 · Cited by 63 · see citing works
Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogs
Gao, Y., Baldessarini, R. J., Kula, N. S., & Neumeyer, J. L. (1990) · Journal of Medicinal Chemistry · doi:10.1021/jm00168a040 · Cited by 60 · see citing works
Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist
Neumeyer, J. L., Gao, Y., Kula, N. S., & Baldessarini, R. J. (1990) · Journal of Medicinal Chemistry · doi:10.1021/jm00174a002 · Cited by 45 · see citing works
Dopamine D2 receptor radiotracers [11C](+)-PHNO and [3H]raclopride are indistinguishably inhibited by D2 agonists and antagonists ex vivo
McCormick, P. N., Kapur, S., Seeman, P. M., & Wilson, A. A. (2007) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2007.08.005 · Cited by 45 · see citing works
Amphetamine pretreatment induces a change in both D2-Receptor density and apparent affinity: a [11C]raclopride positron emission tomography study in cats.
Ginovart, N., Wilson, A., Houle, S., & Kapur, S. (2004) · Biological Psychiatry · doi:10.1016/j.biopsych.2004.02.019 · Cited by 44 · see citing works
Modulation of voluntary ethanol consumption by beta‐arrestin 2
Björk, K., Rimondini, R., Hansson, A. C., Terasmaa, A., Hyytiä, P., Heilig, M. A., & Sommer, W. H. (2008) · The FASEB Journal · doi:10.1096/fj.07-102442 · Cited by 41 · see citing works
Self-citation
Arrestin3 mediates D2dopamine receptor internalization
Skinbjerg, M., Ariano, M. A., Thorsell, A., Heilig, M. A., Halldin, C., Innis, R. B., & Sibley, D. R. (2009) · Synapse · doi:10.1002/syn.20636 · Cited by 37 · see citing works
Self-citation
Integration of a microwave reactor with synthia to provide a fully automated radiofluorination module
Lazarova, N., Siméon, F. G., Musachio, J. L., Lu, S., & Pike, V. W. (2007) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.1196 · Cited by 36 · see citing works
Self-citation
Dopamine D2/3receptor occupancy of apomorphine in the nonhuman primate brain—A comparative PET study with [11C]raclopride and [11C]MNPA
Finnema, S. J., Halldin, C., Bang‐Andersen, B., Gulyás, B. Z., Bundgaard, C., Wikström, H., & Farde, L. (2009) · Synapse · doi:10.1002/syn.20615 · Cited by 33 · see citing works
Self-citation
Amphetamine‐induced dopamine release: Duration of action as assessed with the D2/3 receptor agonist radiotracer (––)‐N‐[11C]propyl‐norapomorphine ([11C]NPA) in an anesthetized nonhuman primate
Narendran, R., Slifstein, M., Hwang, D., Hwang, Y., Scher, E., Reeder, S. A., Martinez, D., & Laruelle, M. (2007) · Synapse · doi:10.1002/syn.20346 · Cited by 32 · see citing works
Critical reevaluation of spiperone and benzamide binding to dopamine D2 receptors: evidence for identical binding sites
Malmberg, Å., Jerning, E., & Mohell, N. (1996) · European Journal of Pharmacology · doi:10.1016/0014-2999(96)00080-5 · Cited by 28 · see citing works
Ex vivo [11C]‐(+)‐PHNO binding is unchanged in animal models displaying increased high‐affinity states of the D2receptor in vitro
McCormick, P. N., Kapur, S., Reckless, G. E., & Wilson, A. A. (2009) · Synapse · doi:10.1002/syn.20671 · Cited by 23 · see citing works
A two‐step one‐pot radiosynthesis of the potent dopamine D2/D3 agonist PET radioligand [11C]MNPA
Steiger, C., Finnema, S. J., Raus, L., Schou, M., Nakao, R., Suzuki, K., Pike, V. W., Wikström, H., & Halldin, C. (2009) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.1583 · Cited by 10 · see citing works
Self-citation
Dopamine D2/D3 receptor occupancy of apomorphine evaluated with the agonist radioligand [11C]MNPA and the antagonist radioligand [11C]Raclopride. A PET evaluation in the non-human primate brain
Finnema, S. J., Bang‐Andersen, B., Farde, L., Gulyás, B. Z., Wikström, H. V., & Halldin, C. (2006) · NeuroImage · doi:10.1016/j.neuroimage.2006.04.106 · Cited by 5 · see citing works
Self-citation
Impact of dopamine D2 receptor internalization on binding parameters of D2 PET radiotracers
Laruelle, M. A., Guo, N., Guo, W. X., Jiang, M., Schieren, I., Abi‐Dargham, A., Javitch, J. A., & Rayport, S. (2008) · NeuroImage · doi:10.1016/j.neuroimage.2008.04.210 · Cited by 4 · see citing works

Flagged first, then by citations

2 of the 36 references couldn’t be matched to a known paper.

Research works printed but not linked: 1

Bjurling P Reineck R Westerburg G Gee AD Sutcliffe J Långström B Link JM Ruth TJ 1995 Synthia, a compact radiochemistry system for automated production of radiopharmaceuticals Proceedings - Sixth Workshop on Targetry and Target Chemistry TRIUMF, Vancouver 282 284

Sorted by citations

The pharmacology of amphetamine and methylphenidate: Relevance to the neurobiology of attention-deficit/hyperactivity disorder and other psychiatric comorbidities
Faraone, S. V. (2018) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2018.02.001 · Cited by 631 · see citing works
Evidence that sleep deprivation downregulates dopamine D2R in ventral striatum in the human brain
Volkow, N. D., Tomasi, D., Wang, G.-J., Telang, F., Fowler, J. S., Logan, J., Benveniste, H., Kim, R., Thanos, P. K., & Ferré, S. (2012) · The Journal of Neuroscience · doi:10.1523/jneurosci.0045-12.2012 · Cited by 254 · see citing works
Neuromelanin-sensitive MRI as a noninvasive proxy measure of dopamine function in the human brain
Cassidy, C., Zucca, F. A., Girgis, R. R., Baker, S. C., Weinstein, J. J., Sharp, M. E., Bellei, C., Valmadre, A., Vanegas‐Arroyave, N., Kegeles, L. S., et al. (2019) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1807983116 · Cited by 247 · see citing works
Imaging dopamine transmission in cocaine dependence: link between neurochemistry and response to treatment
Martinez, D., Carpenter, K. M., Liu, F., Slifstein, M., Broft, A., Friedman, A. C., Kumar, D., Van Heertum, R., Kleber, H. D., & Nunes, E. (2011) · American Journal of Psychiatry · doi:10.1176/appi.ajp.2010.10050748 · Cited by 212 · see citing works
Molecular imaging of microglia/macrophages in the brain
Venneti, S., Lopresti, B. J., & Wiley, C. A. (2012) · Glia · doi:10.1002/glia.22357 · Cited by 189 · see citing works
Deficits in dopamine D2 receptors and pre-synaptic dopamine in heroin dependence: commonalities and differences with other types of addiction
Martinez, D., Saccone, P., Liu, F., Slifstein, M., Orlowska, D., Grassetti, A., Cook, S., Broft, A., Heertum, R. V. V., & Comer, S. (2011) · Biological Psychiatry · doi:10.1016/j.biopsych.2011.08.024 · Cited by 153 · see citing works
Within-Subject Comparison of [11C]-( + )-PHNO and [11C]raclopride Sensitivity to Acute Amphetamine Challenge in Healthy Humans
Shotbolt, P., Tziortzi, A., Searle, G., Colasanti, A., van der Aart, J., Abanades, S., Plisson, C., Miller, S. R., Huiban, M., Beaver, J., et al. (2012) · Journal of Cerebral Blood Flow and Metabolism · doi:10.1038/jcbfm.2011.115 · Cited by 156 · see citing works
Measuring Endogenous 5-HT Release by Emission Tomography: Promises and Pitfalls
Paterson, L. M., Tyacke, R. J., Nutt, D., & Knudsen, G. M. (2010) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.2010.104 · Cited by 145 · see citing works
Quantitative imaging of protein targets in the human brain with PET
Gunn, R. N., Slifstein, M., Searle, G. E., & Price, J. C. (2015) · Physics in Medicine and Biology · doi:10.1088/0031-9155/60/22/r363 · Cited by 85 · see citing works
Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders
Newman‐Tancredi, A., Depoortère, R., Kleven, M. S., Kołaczkowski, M., & Zimmer, L. (2021) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2021.107937 · Cited by 83 · see citing works
Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism
Vauquelin, G., Bostoen, S., Vanderheyden, P., & Seeman, P. M. (2012) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-012-0734-2 · Cited by 80 · see citing works
Application of cross-species PET imaging to assess neurotransmitter release in brain
Finnema, S., Scheinin, M., Shahid, M., Lehto, J., Borroni, E., Bang-Andersen, B., Sallinen, J., Wong, E. H. F., Farde, L., Halldin, C., et al. (2015) · Psychopharmacology · doi:10.1007/s00213-015-3938-6 · Cited by 69 · see citing works
Self-citation
Significant decreases in frontal and temporal [11C]-raclopride binding after THC challenge
Stokes, P. R. A., Egerton, A., Watson, B., Reid, A., Breen, G., Lingford-Hughes, A., Nutt, D., & Mehta, M. (2010) · NeuroImage · doi:10.1016/j.neuroimage.2010.04.274 · Cited by 75 · see citing works
Dopaminergic Neurotransmission in the Human Brain
Ko, J. H., & Strafella, A. P. (2011) · The Neuroscientist · doi:10.1177/1073858411401413 · Cited by 69 · see citing works
Imaging Agonist-Induced D2/D3 Receptor Desensitization and Internalization In Vivo with PET/fMRI
Sander, C., Hooker, J., Catana, C., Rosen, B., & Mandeville, J. (2016) · Neuropsychopharmacology · doi:10.1038/npp.2015.296 · Cited by 72 · see citing works
A receptor-based model for dopamine-induced fMRI signal
Mandeville, J. B., Sander, C. Y. M., Jenkins, B. G., Hooker, J. M., Catana, C., Vanduffel, W., Alpert, N. M., Rosen, B. R., & Normandin, M. D. (2013) · NeuroImage · doi:10.1016/j.neuroimage.2013.02.036 · Cited by 65 · see citing works
Prefrontal dopaminergic receptor abnormalities and executive functions in Parkinson's disease
Ko, J. H., Antonelli, F., Monchi, O., Ray, N. J., Rusjan, P., Houle, S., Lang, A. E., Christopher, L., & Strafella, A. P. (2012) · Human Brain Mapping · doi:10.1002/hbm.22006 · Cited by 61 · see citing works
Absolute abundances and affinity states of dopamine receptors in mammalian brain: A review
Cumming, P. D. (2011) · Synapse · doi:10.1002/syn.20916 · Cited by 59 · see citing works
Imaging the high-affinity state of the dopamine D2 receptor in vivo: Fact or fiction?
Skinbjerg, M., Sibley, D., Javitch, J., & Abi-Dargham, A. (2011) · Biochemical Pharmacology · doi:10.1016/j.bcp.2011.09.008 · Cited by 63 · see citing works
Self-citation
The chemical tools for imaging dopamine release
Post, M. R., & Sulzer, D. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.04.005 · Cited by 54 · see citing works
Imaging dopamine transmission in the frontal cortex: a simultaneous microdiaysis and [11C]FLB 457 PET study
Narendran, R., Jedema, H., Lopresti, B., Mason, N., Gurnsey, K., Ruszkiewicz, J., Chen, C.-M., Deuitch, L., Frankle, W., & Bradberry, C. (2013) · Molecular Psychiatry · doi:10.1038/mp.2013.9 · Cited by 39 · see citing works
Quantitative Rodent Brain Receptor Imaging
Herfert, K., Mannheim, J. G., Kuebler, L., Marciano, S., Amend, M., Parl, C., Napieczyńska, H., Maier, F. M., Vega, S. C., & Pichler, B. J. (2019) · Molecular Imaging and Biology · doi:10.1007/s11307-019-01368-9 · Cited by 47 · see citing works
Is There a Role for GPCR Agonist Radiotracers in PET Neuroimaging?
Colom, M., Vidal, B., & Zimmer, L. (2019) · Frontiers in Molecular Neuroscience · doi:10.3389/fnmol.2019.00255 · Cited by 44 · see citing works
Measuring Dopamine Synaptic Transmission with Molecular Imaging and Pharmacological Challenges: The State of the Art
Laruelle, M. (2012) · Neuromethods · doi:10.1007/7657_2012_45 · Cited by 40 · see citing works
Agonist high- and low-affinity states of dopamine D2 receptors: methods of detection and clinical implications
van Wieringen, J., Booij, J., Shalgunov, V., Elsinga, P., & Michel, M. (2012) · Naunyn-Schmiedeberg's Archives of Pharmacology · doi:10.1007/s00210-012-0817-0 · Cited by 40 · see citing works
Assessment of serotonin release capacity in the human brain using dexfenfluramine challenge and [18F]altanserin positron emission tomography
Quednow, B. B., Treyer, V., Hasler, F., Doerig, N., Wyss, M. T., Burger, C., Rentsch, K., Westera, G., Schubiger, P. A., Buck, A., et al. (2011) · NeuroImage · doi:10.1016/j.neuroimage.2011.09.045 · Cited by 35 · see citing works
Dysfunctional Brain Networks and Genetic Risk for Schizophrenia: Specific Neurotransmitter Systems
Hirvonen, J., & Hietala, J. (2011) · CNS Neuroscience & Therapeutics · doi:10.1111/j.1755-5949.2010.00223.x · Cited by 37 · see citing works
Noninvasive Nuclear Imaging Enables the In Vivo Quantification of Striatal Dopamine Receptor Expression and Raclopride Affinity in Mice
Fischer, K., Sossi, V., Schmid, A. M., Thunemann, M., Maier, F. C., Judenhofer, M. S., Mannheim, J. G., Reischl, G., & Pichler, B. J. (2011) · Journal of Nuclear Medicine · doi:10.2967/jnumed.110.086942 · Cited by 34 · see citing works
News and views on in-vivo imaging of neurotransmission using PET and MRI
Sander, C. Y. M., & Hesse, S. (2017) · The Quarterly Journal of Nuclear Medicine and Molecular Imaging · doi:10.23736/s1824-4785.17.03019-9 · Cited by 33 · see citing works
Mechanistic models enable the rational use ofin vitrodrug-target binding kinetics for better drug effects in patients
de Witte, W. E. A., Wong, Y. C., Nederpelt, I., Heitman, L. H., Danhof, M., van der Graaf, P. H., Gilissen, R., & de Lange, E. C. M. (2015) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2016.1100163 · Cited by 32 · see citing works
PET imaging of dopamine-D2 receptor internalization in schizophrenia
Weinstein, J., van de Giessen, E. M., Rosengard, R., Xu, X., Ojeil, N., Brucato, G., Gil, R. B., Kegeles, L., Laruelle, M., Slifstein, M., et al. (2017) · Molecular Psychiatry · doi:10.1038/mp.2017.107 · Cited by 26 · see citing works
Dopamine agonist radioligand binds to both D2High and D2Low receptors, explaining why alterations in D2High are not detected in human brain scans
Seeman, P. M. (2011) · Synapse · doi:10.1002/syn.20987 · Cited by 32 · see citing works
Vulnerability to psychotogenic effects of ketamine is associated with elevated D2/3-receptor availability
Vernaleken, I., Klomp, M., Moeller, O., Raptis, M., Nagels, A., Rösch, F., Schaefer, W. M., Cumming, P. D., & Gründer, G. (2012) · The International Journal of Neuropsychopharmacology · doi:10.1017/s1461145712000764 · Cited by 31 · see citing works
Isoflurane Anaesthesia Differentially Affects the Amphetamine Sensitivity of Agonist and Antagonist D2/D3 Positron Emission Tomography Radiotracers: Implications for In Vivo Imaging of Dopamine Release
McCormick, P. N., Ginovart, N., & Wilson, A. A. (2010) · Molecular Imaging and Biology · doi:10.1007/s11307-010-0380-3 · Cited by 30 · see citing works
Catecholamines
Gnegy, M. E. (2012) · Elsevier eBooks · doi:10.1016/b978-0-12-374947-5.00014-6 · Cited by 28 · see citing works
Acute and Sustained Effects of Methylphenidate on Cognition and Presynaptic Dopamine Metabolism: An [18F]FDOPA PET Study
Schabram, I., Henkel, K., Shali, S. M., Dietrich, C., Schmaljohann, J., Winz, O., Prinz, S., Rademacher, L., Neumaier, B., Felzen, M., et al. (2014) · Journal of Neuroscience · doi:10.1523/jneurosci.1560-14.2014 · Cited by 27 · see citing works
Validation of the Octamouse for Simultaneous 18F-Fallypride Small-Animal PET Recordings from 8 Mice
Rominger, A., Mille, E., Zhang, S., Böning, G., Förster, S., Nowak, S., Gildehaus, F. J., Wängler, B., Bartenstein, P., & Cumming, P. D. (2010) · Journal of Nuclear Medicine · doi:10.2967/jnumed.110.078451 · Cited by 26 · see citing works
Quantification of dopamine D2/3 receptors in rat brain using factor analysis corrected [18F]Fallypride images
Millet, P., Sallanon, M. M., Tournier, B. B., Dumas, N., Charnay, Y., Ibáñez, V., & Ginovart, N. (2012) · NeuroImage · doi:10.1016/j.neuroimage.2012.05.075 · Cited by 26 · see citing works
Hunting for the high‐affinity state of G‐protein‐coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging
Shalgunov, V., van Waarde, A., Booij, J., Michel, M. C., Dierckx, R., & Elsinga, P. H. (2018) · Medicinal Research Reviews · doi:10.1002/med.21552 · Cited by 24 · see citing works
Trans-Modulation of the Somatostatin Type 2A Receptor Trafficking by Insulin-Regulated Aminopeptidase Decreases Limbic Seizures
Bundel, D. D., Fafouri, A., Csaba, Z., Loyens, E., Lebon, S., Ghouzzi, V. E., Peineau, S., Vodjdani, G., Kiagiadaki, F., Aourz, N., et al. (2015) · Journal of Neuroscience · doi:10.1523/jneurosci.0476-15.2015 · Cited by 20 · see citing works
Human Biodistribution and Dosimetry of 11C-CUMI-101, an Agonist Radioligand for Serotonin-1A Receptors in Brain
Hines, C. S., Liow, J., Zanotti‐Fregonara, P., Hirvonen, J., Morse, C. L., Pike, V. W., & Innis, R. B. (2011) · PLoS ONE · doi:10.1371/journal.pone.0025309 · Cited by 18 · see citing works
Self-citation
Immediate and Persistent Effects of Salvinorin A on the Kappa Opioid Receptor in Rodents, Monitored In Vivo with PET
Placzek, M. S., de Bittner, G. C. V., Wey, H., Lukas, S. E., & Hooker, J. M. (2015) · Neuropsychopharmacology · doi:10.1038/npp.2015.159 · Cited by 17 · see citing works
Is it Pre- or Postsynaptic? Imaging Striatal Dopamine Excess in Schizophrenia
Slifstein, M., & Abi‐Dargham, A. (2018) · Biological Psychiatry · doi:10.1016/j.biopsych.2018.02.015 · Cited by 16 · see citing works
Striatal phosphodiesterase 10A availability is altered secondary to chronic changes in dopamine neurotransmission
Ooms, M., Celen, S., Hoogt, R. D., Lenaerts, I., Liebregts, J., Vanhoof, G., Langlois, X., Postnov, A. A., Koole, M. J. B., Verbruggen, A., et al. (2016) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-016-0005-5 · Cited by 15 · see citing works
Quinpirole elicits differential in vivo changes in the pre- and postsynaptic distributions of dopamine D2 receptors in mouse striatum: relation to cannabinoid-1 (CB1) receptor targeting
Lane, D., Chan, J., Fitzgerald, M. L., Kearn, C. S., Mackie, K., & Pickel, V. M. (2011) · Psychopharmacology · doi:10.1007/s00213-011-2553-4 · Cited by 14 · see citing works
Repeated application of Modafinil and Levodopa reveals a drug-independent precise timing of spatial working memory modulation
Bezu, M., Shanmugasundaram, B., Lübec, G., & Korz, V. (2016) · Behavioural Brain Research · doi:10.1016/j.bbr.2016.06.003 · Cited by 14 · see citing works
The influence of different cellular environments on PET radioligand binding: An application to D2/3-dopamine receptor imaging
Quelch, D. R., Withey, S. L., Nutt, D., Tyacke, R. J., & Parker, C. A. (2014) · Neuropharmacology · doi:10.1016/j.neuropharm.2014.05.040 · Cited by 13 · see citing works
Cocaine: Mechanism and Effects in the Human Brain
Trifilieff, P., & Martinez, D. (2014) · Elsevier eBooks · doi:10.1016/b978-0-12-418679-8.00005-8 · Cited by 6 · see citing works
Measuring amphetamine‐induced dopamine release in humans: A comparative meta‐analysis of [11C]‐raclopride and [11C]‐(+)‐PHNO studies
Caravaggio, F., Porco, N., Kim, J., Torres-Carmona, E., Brown, E. E., Iwata, Y., Nakajima, S., Gerretsen, P., Remington, G., & Graff-Guerrero, A. (2021) · Synapse · doi:10.1002/syn.22195 · Cited by 12 · see citing works
Defect of TIMP4 Is Associated with High Myopia and Participates in Rat Ocular Development in a Dose-Dependent Manner
Zhou, W., Jiang, Z., Yi, Z., Ouyang, J., Li, X., Zhang, Q., & Wang, P. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms242316928 · Cited by 10 · see citing works
A local-neighborhood Lassen plot filter for creating occupancy and non-displaceable binding images
de Laat, B., & Morris, E. D. (2020) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x20950486 · Cited by 9 · see citing works
Acute effect of intravenously applied alcohol in the human striatal and extrastriatal D2/D3dopamine system
Pfeifer, P., Tüscher, O., Buchholz, H. G., Gründer, G., Vernaleken, I., Paulzen, M., Zimmermann, U. S., Maus, S., Lieb, K., Eggermann, T., et al. (2016) · Addiction Biology · doi:10.1111/adb.12424 · Cited by 9 · see citing works
Partial volume correction of PET image data using geometric transfer matrices based on uniform B-splines
Mandeville, J. B., Efthimiou, N., Weigand‐Whittier, J., Hardy, E. E., Knudsen, G. M., Jørgensen, L. M., & Chen, Y. I. (2024) · Physics in Medicine and Biology · doi:10.1088/1361-6560/ad22a0 · Cited by 8 · see citing works
Abnormal dopamine receptor signaling allows selective therapeutic targeting of neoplastic progenitors in AML patients
Aslostovar, L., Boyd, A. L., Benoit, Y. D., Lu, J. D., García‐Rodríguez, J. L., Nakanishi, M., Porras, D. P., Reid, J. C., Mitchell, R. R., Leber, B. F., et al. (2021) · Cell Reports Medicine · doi:10.1016/j.xcrm.2021.100202 · Cited by 8 · see citing works
The Role of a Dopamine-Dependent Limbic–Motor Network in Sensory Motor Processing in Parkinson Disease
Mann, L. G., Servant, M., Hay, K. R., Song, A. K., Trujillo, P., Yan, B., Kang, H., Zald, D. H., Donahue, M. J., Logan, G. D., et al. (2023) · Journal of Cognitive Neuroscience · doi:10.1162/jocn_a_02048 · Cited by 7 · see citing works
The Chronic Oral Administration of Clobenzorex or Amphetamine Decreases Motor Behavior and Induces Glial Activation in the Striatum Without Dopaminergic Degeneration
del Rosal, G. D. A., Limón, I. D., Martínez, I., & Patricio-Martínez, A. (2021) · Neurotoxicity Research · doi:10.1007/s12640-021-00395-1 · Cited by 6 · see citing works
PET and SPECT Imaging of the Central Dopamine System in Humans
Booij, J., van Wieringen, J., van de Giessen, E. M., Knol, R., & Finnema, S. (2020) · PET and SPECT of Neurobiological Systems · doi:10.1007/978-3-642-42014-6_10 · Cited by 6 · see citing works
Effect of mazindol on extracellular dopamine concentration in human brain measured by PET
Sakayori, T., Tateno, A., Arakawa, R., Ikeda, Y., Suzuki, H., & Okubo, Y. (2014) · Psychopharmacology · doi:10.1007/s00213-013-3392-2 · Cited by 6 · see citing works
The role of beta-arrestin2 in shaping fMRI BOLD responses to dopaminergic stimulation
Sahlholm, K., Ielacqua, G. D., Xu, J., Jones, L. A., Schlegel, F., Mach, R. H., Rudin, M., & Schroeter, A. (2017) · Psychopharmacology · doi:10.1007/s00213-017-4609-6 · Cited by 5 · see citing works
Agonist signalling properties of radiotracers used for imaging of dopamine D2/3 receptors
van Wieringen, J., Michel, M. C., Janssen, H. M., Janssen, A. G. M., Elsinga, P. H., & Booij, J. (2014) · EJNMMI Research · doi:10.1186/s13550-014-0053-3 · Cited by 4 · see citing works
Neurochemical Imaging of Addictive Disorders
Broft, A. I., & Martínez, D. (2012) · Neuromethods · doi:10.1007/7657_2012_48 · Cited by 4 · see citing works
Dopamine Receptors and Dopamine Release
Kessler, R. (2014) · Elsevier eBooks · doi:10.1016/b978-0-12-418677-4.00012-9 · Cited by 1 · see citing works
Prolonged Amphetamine Exposures Increase the Endogenous Human Dopamine Receptors 2 at the Cellular Membrane in Cells Lacking the Dopamine Transporter
Nawaratne, V., McLaughlin, S. P., Mayer, F. P., Gichi, Z., Mastriano, A., & Carvelli, L. (2021) · Frontiers in Cellular Neuroscience · doi:10.3389/fncel.2021.681539 · Cited by 3 · see citing works
Dopamine Receptor Imaging in Schizophrenia: Focus on Genetic Vulnerability
Hirvonen, J., & Hietala, J. (2014) · Elsevier eBooks · doi:10.1016/b978-0-12-418677-4.00013-0 · Cited by 4 · see citing works
PET and SPECT Imaging of the Central Dopamine System in Humans
Booij, J., van Wieringen, J., van de Giessen, E., Knol, R. J. J., & Finnema, S. J. (2020) · Springer eBooks · doi:10.1007/978-3-030-53176-8_11 · Cited by 3 · see citing works
Evidence for Dopamine Abnormalities Following Acute Methamphetamine Exposure Assessed by Neuromelanin-Sensitive Magnetic Resonance Imaging
Tang, F., Liu, H., Zhang, X. J., Zheng, H., Dai, Y. M., Zheng, L. Y., Yang, W. H., Du, Y. Y., & Liu, J. (2022) · Frontiers in Aging Neuroscience · doi:10.3389/fnagi.2022.865825 · Cited by 2 · see citing works
Amphetamine pretreatment blunts dopamine-induced D2/D3-receptor occupancy by an arrestin-mediated mechanism: A PET study in internalization compromised mice
Mandeville, J. B., Weigand‐Whittier, J., Wey, H., & Chen, Y. I. (2023) · NeuroImage · doi:10.1016/j.neuroimage.2023.120416 · Cited by 2 · see citing works
Design and Synthesis of Novel PET Radiotracers for Imaging Sphingosine-1-Phosphate Receptor 5 (S1PR5) in the Brain
Lang, J., Zhou, W., Huang, T., Jiang, H., Chen, H., Xu, S., Qiu, L., Heady, M., Yu, Y., Brier, M. R., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00881 · Cited by 1 · see citing works
Evaluation of Dopamine Receptor Integrity after Sevo fl urane Exposure in Neonatal Rat Brain Using Positron Emission Tomography
Xuan, Z. (2018) · Global Journal of Anesthesiology · doi:10.17352/2455-3476.000040 · Cited by 1 · see citing works
Neurochemical Imaging in Addiction
Wai, J. M., LEVIN, F. R., & Martínez, D. (2018) · Elsevier eBooks · doi:10.1016/b978-0-323-54856-4.00001-8 · Cited by 1 · see citing works
Evaluation of Dopamine Receptor Integrity after Sevo fl urane Exposure in Neonatal Rat Brain Using Positron Emission Tomography
Zhang, X. (2018) · Global Journal of Anesthesiology · doi:10.17352/gja.000010 · Cited by 1 · see citing works
Differential D 1 and D 2 receptor internalization and recycling induced by amphetamine in vivoPreprint
Hansen, H. D., Schain, M., Deng, H. P., Mandeville, J. B., Rosen, B. R., & Sander, C. Y. M. (2022) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2022.06.10.493955 · Cited by 1 · see citing works
Assessment of Dopamine and Serotonin Release in the Non-Human Primate Brain using PET
Finnema, S. J. (2011) · Figshare
Neural substrates of amphetamine induced impulsive behaviour
Twiston-Davies, F. L. (2013) · White Rose eTheses Online (University of Leeds, The University of Sheffield, University of York)
an Agonist Radioligand for Serotonin-1A Receptors in Brain
Hines, C. S., Liow, J., Zanotti‐Fregonara, P., Hirvonen, J., Morse, C. L., Pike, V. W., & Innis, R. B. (2011)
Self-citation
Microwave-accelerated transformations in synthetic organic & medicinal chemistry
Kallmerten, A. E. (2010) · doi:10.17760/d20001091
A Retrospective on PET and the Amphetamine Paradigm: Validation and Paradoxes
Abi‐Dargham, A. (2013) · Elsevier eBooks · doi:10.1016/b978-0-12-800044-1.00039-8
Imaging of Neurochemical Transmission in the Central Nervous System
Deuitch, L., & Narendran, R. (2014) · Elsevier eBooks · doi:10.1016/b978-0-12-418677-4.00019-1
Molecular Imaging in Schizophrenia
Howes, O. D. (2012) · Neuromethods · doi:10.1007/7657_2012_57
Molecular imaging of dopamine synthesis and release
Shotbolt, J. (2013) · Spiral (Imperial College London) · doi:10.25560/11152
PET studies on the mechanisms of action of antidepressant and antipsychotic drugs
Yang, K. (2017) · Figshare
Applications, Advances, and Limitations of Molecular Imaging of Brain Receptors
Cumming, P. D., Gründer, G., Brinson, Z. S., & Wong, D. F. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-816386-3.00063-6
Current Awareness in Labelled Compounds and Radiopharmaceuticals
(2010) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.1683
Molecular Neuroimaging in Addictive Disorders
London, E. D., & Robertson, C. L. (2017) · doi:10.1093/med/9780190681425.003.0045
The radiotracer [123I]I-FP-CIT binds preferentially to the dopamine transporter expressed at the plasma membrane of nigrostriatal dopaminergic neurons: a new concept
Booij, J., Chahid, Y., Reits, E. A., & Gether, U. (2025) · Annals of Nuclear Medicine · doi:10.1007/s12149-025-02140-6
The Binding of the High Affinity Radioligand Fallypride to the D2-dopamine Receptor is Sensitive to Injected Mass – a PET Study in Rodents
Tóth, M., Tari, L., Nag, S., Qiu, T., Jia, Z., Häggkvist, J., Mukherjee, J., Varrone, A., Halldin, C., & Farde, L. (2026) · Molecular Imaging and Biology · doi:10.1007/s11307-026-02096-7
Self-citation

Amphetamine pretreatment blunts dopamine-induced D2/D3-receptor occupancy by an arrestin-mediated mechanism: A PET study in internalization compromised mice
Mandeville, J. B., Weigand‐Whittier, J., Wey, H., & Chen, Y. I. (2023) · NeuroImage · doi:10.1016/j.neuroimage.2023.120416 · Cited by 2 · see citing works
Impact of D2 receptor internalization on binding affinity of neuroimaging radiotracers
Guo, N., Guo, W., Králíková, M., Jiang, M., Schieren, I., Narendran, R., Slifstein, M., Abi-Dargham, A., Laruelle, M., Javitch, J., et al. (2009) · Neuropsychopharmacology · doi:10.1038/npp.2009.189 · Cited by 88 · see citing works
In vivo evidence for dopamine-mediated internalization of D2-receptors after amphetamine: differential findings with [3H]raclopride versus [3H]spiperone
Sun, W., Ginovart, N., Ko, F., Seeman, P., & Kapur, S. (2003) · Molecular Pharmacology · doi:10.1124/mol.63.2.456 · Cited by 99 · see citing works
Amphetamine pretreatment induces a change in both D2-Receptor density and apparent affinity: a [11C]raclopride positron emission tomography study in cats.
Ginovart, N., Wilson, A., Houle, S., & Kapur, S. (2004) · Biological Psychiatry · doi:10.1016/j.biopsych.2004.02.019 · Cited by 44 · see citing works
Differential D1 and D2 receptor internalization and recycling induced by amphetamine in vivo: a PET/fMRI study
Hansen, H. D., Schain, M., Deng, H., Mandeville, J. B., Rosen, B. R., & Sander, C. Y. M. (2023) · Proceedings on CD-ROM - International Society for Magnetic Resonance in Medicine. Scientific Meeting and Exhibition/Proceedings of the International Society for Magnetic Resonance in Medicine, Scientific Meeting and Exhibition · doi:10.58530/2022/3336

Authors: Skinbjerg, M., Liow, J.-S., Seneca, N., Hong, J., Lu, S., Thorsell, A., Heilig, M., Pike, V. W., Halldin, C., Sibley, D. R., & Innis, R. B.
Affiliations: National Institutes of Health (US)
National Institute on Alcohol Abuse and Alcoholism (US)
Karolinska Institutet (SE)
National Institute of Neurological Disorders and Stroke (US)
Corresponding author: Innis, Robert B.
ORCID: Liow, Jeih-San
Hong, Jinsoo
Lu, Shuiyu
Thorsell, Annika
Heilig, Markus
Pike, Victor W.
Halldin, Christer
Sibley, David R.
Innis, Robert B.
Venue: NeuroImage
Publisher: Elsevier BV
Published: 2010-05
Volume: 50
Issue: 4
Pages: 1402-1407
ISSN: 1053-8119 (ISSN-L)
DOI: 10.1016/j.neuroimage.2010.01.055
PMC: PMC2838946
OpenAlex: W2143378099
Cited by: 86
References: 36
Citations by year: 2026: 1 · 2025: 2 · 2024: 1 · 2023: 3 · 2022: 2 · 2021: 7 · 2020: 2 · 2019: 3 · 2018: 6 · 2017: 5 · 2016: 3 · 2015: 6 · 2014: 9 · 2013: 5 · 2012: 11
FWCI: 4.66
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: NeuroImage (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: Intramural Program of NIMH (Z01-MH-002795-07, Z01-MH-002793)
NINDS (NS002263-33)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords: dopamine D2 receptor, receptor internalization, amphetamine, dopamine release, radioligand binding, receptor trafficking, high-affinity state, small animal PET
MeSH terms: Amphetamine, Animals, Brain, Carbon Radioisotopes, Cell Membrane, Cerebellum, Corpus Striatum, Female, Fluorine Radioisotopes, Male, Naproxen, Time Factors, Dopamine Agents, Receptors, Dopamine D2, Mice, Knockout, Radiopharmaceuticals, Arrestins, Positron-Emission Tomography, Mice

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: a PET study in a receptor internalization-deficient mouse model

Abstract

Integrity signals

Claims the paper makes

Self-check

Cites

Cited by

Related

Record

About these checks