Research Topics
| Michael KilbournSummaryAffiliation: University of Michigan Country: USA Publications
Research Grants
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Detail Information
Publications
Simplified methods for in vivo measurement of acetylcholinesterase activity in rodent brainM R Kilbourn
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109, USA
Nucl Med Biol 26:543-50. 1999..We conclude that certain simple measures of AChE hydrolysis rates for [11C]PMP are suitable for studies where alterations of the peripheral blood metabolism of the tracer are kept to a minimum...- Differential effects of scopolamine on in vivo binding of dopamine transporter and vesicular monoamine transporter radioligands in rat brainMichael R Kilbourn
Department of Radiology, Division of Nuclear Medicine, University of Michigan Medical School, Ann Arbor 48109, USA
Exp Neurol 188:387-90. 2004.... 
Increased in vivo [11C]raclopride binding to brain dopamine receptors in amphetamine-treated ratsMichael R Kilbourn
Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
Eur J Pharmacol 654:254-7. 2011..These results support increased baseline in vivo dopamine D(2) receptor antagonist radioligand binding after repeated amphetamine administration in rats...
Pharmacokinetics of [(18)F]fluoroalkyl derivatives of dihydrotetrabenazine in rat and monkey brainMichael R Kilbourn
Department of Radiology, University of Michigan Medical School, Ann Arbor, MI, USA
Nucl Med Biol 34:233-7. 2007....- Anesthesia increases in vivo N-([18F]fluoroethyl)piperidinyl benzilate binding to the muscarinic cholinergic receptorMichael R Kilbourn
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109 0552, USA
Nucl Med Biol 34:479-82. 2007..These studies demonstrate that anesthesia can produce significant changes in baseline biochemical measures that can obscure even very large effects of pharmacological challenges... - Rapid and differential losses of in vivo dopamine transporter (DAT) and vesicular monoamine transporter (VMAT2) radioligand binding in MPTP-treated miceM R Kilbourn
Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical School, Ann Arbor, Michigan 48109, USA
Synapse 35:250-5. 2000..These studies indicate that the losses of the neuronal membrane and vesicular transporters are not always equal, and do not occur in the same time frame, after administration of the neurotoxin MPTP... - In vivo measures of dopaminergic radioligands in the rat brain: equilibrium infusion studiesMichael R Kilbourn
Division of Nuclear Medicine, Department of Radiology, 3480 Kresge III Bldg, University of Michigan Medical School, Ann Arbor, MI 48109, USA
Synapse 43:188-94. 2002..Equilibrium measures of in vivo radioligand binding, as utilized in this study, offer a quantitative means to evaluate acute and chronic drug effects on in vivo radioligand binding in the rat brain... - N-[11C]methylpiperidine esters as acetylcholinesterase substrates: an in vivo structure-reactivity studyM R Kilbourn
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109, USA
Nucl Med Biol 25:755-60. 1998..This study has identified simple methods to both increase and decrease the in vivo reactivity of piperidinyl esters toward acetylcholinesterase... - Long-term reproducibility of in vivo measures of specific binding of radioligands in rat brainMichael R Kilbourn
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
Nucl Med Biol 31:591-5. 2004..17+/-0.39, N=52), again irrespective of radionuclide or sex. These studies demonstrate that use of a consistent in vivo technique can provide reliable measures of specific binding of radioligands to high affinity sites in the rat brain... - Rat pancreas uptake of [11C]dihydrotetrabenazine stereoisomersMichael R Kilbourn
University of Michigan Medical School, Ann Arbor, MI 48109, USA
Nucl Med Biol 37:869-71. 2010..These studies indicate that the inactive isomer of DTBZ does not provide a mechanism for defining the nonspecific binding of (+)-DTBZ in rat pancreas... - In vivo [11C]dihydrotetrabenazine binding in rat striatum: sensitivity to dopamine concentrationsMichael R Kilbourn
Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
Nucl Med Biol 37:3-8. 2010.... - Reduced MPTP neurotoxicity in striatum of the mutant mouse totteringM R Kilbourn
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109, USA
Synapse 30:205-10. 1998..The tottering mutant does, however, offer another animal model to examine the biochemical features responsible for MPTP toxicity... - In vivo binding of (+)-alpha-[3H]dihydrotetrabenazine to the vesicular monoamine transporter of rat brain: bolus vs. equilibrium studiesM Kilbourn
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109, USA
Eur J Pharmacol 331:161-8. 1997..Both infusion and bolus injection methods give acceptable in vivo measures of (+)-alpha-[3H]dihydrotetrabenazine binding to the vesicular monoamine transporter of rat brain... - Positron emission tomography imaging of (2R,3R)-5-[(18)F]fluoroethoxybenzovesamicol in rat and monkey brain: a radioligand for the vesicular acetylcholine transporterMichael R Kilbourn
Department of Radiology, University of Michigan School of Medicine, Ann Arbor, 48109, USA
Nucl Med Biol 36:489-93. 2009..The regional brain distribution of (2R,3R)-5-[(18)F]fluoroethoxy-benzovesamicol ((-)-[(18)F]FEOBV), a radioligand for the vesicular acetylcholine transporter (VAChT), was examined in vivo in mice, rats and rhesus monkeys... - Behavioral and neurochemical consequences of long-term intravenous self-administration of MDMA and its enantiomers by rhesus monkeysWilliam E Fantegrossi
Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48101 0632, USA
Neuropsychopharmacology 29:1270-81. 2004..The reinforcing effects of MDMA are selectively attenuated by chronic MDMA self-administration, although this behavioral change appears to occur in the absence of any frank neurochemical correlates of toxicity... - In vivo imaging of vesicular monoamine transporter 2 in pancreas using an (18)F epoxide derivative of tetrabenazineHank F Kung
Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
Nucl Med Biol 35:825-37. 2008..The hydrolyzable epoxide group of (+)4 may provide a mechanism for shifting biodistribution from liver to kidney, thus reducing the background signal... - The role of species-dependent metabolism in the regional brain retention of 18F-labeled muscarinic acetylcholine receptor ligandsM B Skaddan
Department of Radiology, University of Michigan Medical School, B1G412 University Hospital, Ann Arbor, MI 48109-0552, USA
Nucl Med Biol 28:753-9. 2001..Our findings emphasize the importance of metabolite analysis in multiple species when developing novel radiopharmaceuticals for in vivo use... - Mutant mouse strains as models for in vivo radiotracer evaluations: [11C]methoxytetrabenazine ([11C]MTBZ) in tottering miceM R Kilbourn
Department of Internal Medicine, University of Michigan School of Medicine, Ann Arbor 48109, USA
Nucl Med Biol 22:565-7. 1995.... - Visualizing pancreatic beta-cell mass with [11C]DTBZNorman Ray Simpson
Department of Radiology, Columbia University Medical School, New York, NY 10032, USA
Nucl Med Biol 33:855-64. 2006.... - [18F]fluoroethoxy-benzovesamicol, a PET radiotracer for the vesicular acetylcholine transporter and cholinergic synapsesG K Mulholland
Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109 0552, USA
Synapse 30:263-74. 1998..These studies show FEOBV maps cholinergic areas with high specificity in vivo, and may provide a noninvasive means to safely and accurately gauge the functional integrity of cholinergic synapses in man using PET... - Striatal [11C]dihydrotetrabenazine and [11C]methylphenidate binding in Tourette syndromeR L Albin
Geriatrics Research, Education, and Clinical Center, Ann Arbor VAMC, Ann Arbor, MI, USA
Neurology 72:1390-6. 2009..Prior molecular imaging studies of nigrostriatal dopaminergic terminal markers report conflicting results. Our goal was to characterize the distribution of nigrostriatal dopaminergic terminals in subjects with TS... - Assessment of muscarinic receptor concentrations in aging and Alzheimer disease with [11C]NMPB and PETJ K Zubieta
Department of Psychiatry, The University of Michigan, Neuroscience Building, 1103 East Huron Street, Ann Arbor, MI 48104 1687, USA
Synapse 39:275-87. 2001..After normalization, no regional changes in muscarinic receptor concentrations were observed in AD... - Increased ventral striatal monoaminergic innervation in Tourette syndromeR L Albin
Department of Neurology, The University of Michigan Medical School, Ann Arbor, USA
Neurology 61:310-5. 2003..Excessive striatal dopaminergic innervation is suggested to underlie Tourette syndrome (TS). Prior imaging and postmortem studies yield conflicting data... - Regional mu opioid receptor regulation of sensory and affective dimensions of painJ K Zubieta
Department of Psychiatry and Mental Health Research Institute, Medical School, The University of Michigan, Ann Arbor, MI 48104 1687, USA
Science 293:311-5. 2001..These data demonstrate the central role of the mu-opioid receptors and their endogenous ligands in the regulation of sensory and affective components of the pain experience... - High vesicular monoamine transporter binding in asymptomatic bipolar I disorder: sex differences and cognitive correlatesJ K Zubieta
Department of Psychiatry, University of Michigan, Ann Arbor, 48104 1687, USA
Am J Psychiatry 157:1619-28. 2000..In this study the authors examined the possibility that trait-related abnormalities in the concentration of monoaminergic synaptic terminals may be present in patients with asymptomatic bipolar disorder type I... - Dual-[11C]tracer single-acquisition positron emission tomography studiesR A Koeppe
Division of Nuclear Medicine, Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, USA
J Cereb Blood Flow Metab 21:1480-92. 2001..The authors conclude that dual-tracer single-scan PET is feasible, yields accurate estimates of multiple neuropharmacologic measures, and can be implemented with a number of different radiotracer pairs... - In vivo mapping of cerebral acetylcholinesterase activity in aging and Alzheimer's diseaseD E Kuhl
Division of Nuclear Medicine, University of Michigan, Ann Arbor, USA
Neurology 52:691-9. 1999..To validate an in vivo method for mapping acetylcholinesterase (AChE) activity in human brain, preparatory to monitoring inhibitor therapy in AD... - Synthesis of 1-[11C]methylpiperidin-4-yl propionate ([11C]PMP) for in vivo measurements of acetylcholinesterase activityS E Snyder
Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109 0028, USA
Nucl Med Biol 25:751-4. 1998..The total synthesis time from end-of-bombardment was 35 min. [11C]PMP can thus be reliably prepared for routine clinical studies of acetylcholinesterase in human brain using positron emission tomography... - Imaging the vesicular monoamine transporterK A Frey
Departments of Radiology and Neurology, University of Michigan, Ann Arbor, Michigan 48109-0028, USA
Adv Neurol 86:237-47. 2001..This methodology appears particularly suited to the objective measure of PD severity and of its progression. Such measures will be indispensable in the search for disease-modifying effects of PD therapy... - Iodine-125 and fluorine-18 labeled aryl-1,4-dialkylpiperazines: potential radiopharmaceuticals for in vivo study of the dopamine uptake systemM E Van Dort
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109
Int J Rad Appl Instrum A 43:671-80. 1992..These studies suggest that development of new radiopharmaceuticals based on the GBR 12935 structure cannot be based solely on considerations of in vitro binding affinities... - Direct simultaneous production of [15O]water and [13N]ammonia or [18F]fluoride ion by 26 MeV proton irradiation of a double chamber water targetG K Mulholland
Division of Nuclear Medicine, University of Michigan, Ann Arbor 48109
Int J Rad Appl Instrum A 41:1193-9. 1990.... - Multiphase extraction: rapid phase-transfer of [18F]fluoride ion for nucleophilic radiolabeling reactionsD M Jewett
Department of Internal Medicine, University of Michigan Medical School, Ann Arbor 48109 0552
Int J Rad Appl Instrum A 39:1109-11. 1988..A wide range of ion-pairs based on K+ or NH+4 cryptands or quaternary ammonium salts can be employed. The method was applied to the synthesis of [18F]FDG... - [18F]fluorination/decarbonylation: new route to aryl [18F]fluoridesP K Chakraborty
Department of Internal Medicine, University of Michigan, Ann Arbor 48109
Int J Rad Appl Instrum A 42:1209-13. 1991.... - In vivo evaluation of new carfentanil-based radioligands for the mu opiate receptorDouglas M Jewett
Division of Nuclear Medicine, Department of Radiology, University of Michigan School of Medicine, Ann Arbor, MI 48109, USA
Nucl Med Biol 31:321-5. 2004.... - Determination of residual Kryptofix 2.2.2 levels in [18F]-labeled radiopharmaceuticals for human usePeter J H Scott
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
Appl Radiat Isot 65:1359-62. 2007.... - Characterization of optically resolved 9-fluoropropyl-dihydrotetrabenazine as a potential PET imaging agent targeting vesicular monoamine transportersMei Ping Kung
Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
Nucl Med Biol 34:239-46. 2007..From these findings, we conclude that [(18)F]FP-(+)-DTBZ is a sensitive and selective tracer for VMAT2 binding sites and it may be useful for in vivo evaluation of diseases relating to changes of monoamine neuronal integrity... - 5-tert-Butyl-2-(4'-[18F]fluoropropynylphenyl)-1,3-dithiane oxides: potential new GABA A receptor radioligandsXuehe Li
Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
Nucl Med Biol 35:549-59. 2008.... - Imaging butyrylcholinesterase activity in Alzheimer's diseaseDavid E Kuhl
Ann Neurol 60:746. 2006 - N-[(18)F]Fluoroethylpiperidinyl, N-[(18)F]fluoroethylpiperidinemethyl and N-[(18)F]fluoroethylpyrrolidinyl esters as radiotracers for acetylcholinesteraseXia Shao
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical Center, Ann Arbor, MI 48109, USA
Nucl Med Biol 30:491-500. 2003..Based on metabolism in mouse blood and PET time-activity curves in rats, two radiotracers were identified as potential candidates for further in vivo evaluation in higher species... - In vivo imaging of beta-cell mass in rats using 18F-FP-(+)-DTBZ: a potential PET ligand for studying diabetes mellitusMei Ping Kung
Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
J Nucl Med 49:1171-6. 2008..In this article, 9-fluoropropyl-(+)-dihydrotetrabenazine (FP-(+)-DTBZ), which is a VMAT2 imaging agent, was evaluated as a PET agent for estimating BCM in vivo... - Sensitivity of [11C]N-methylpyrrolidinyl benzilate ([11C]NMPYB) to endogenous acetylcholine: PET imaging vs tissue sampling methodsBing Ma
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, 3480 Kresge III Building, Ann Arbor, MI 48109, USA
Nucl Med Biol 31:393-7. 2004.... - Positron emission tomography of monoaminergic vesicular binding in aging and Parkinson diseaseNicolaas I Bohnen
Department of Radiology, Division of Nuclear Medicine, The University of Michigan Medical School, Ann Arbor, 48109 0028, USA
J Cereb Blood Flow Metab 26:1198-212. 2006..We conclude that (+)-[(11)C]DTBZ-PET imaging displays many properties necessary of a PD biomarker... - N-methylpiperidinemethyl, N-methylpyrrolidyl and N-methylpyrrolidinemethyl esters as PET radiotracers for acetylcholinesterase activityXia Shao
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical Center, Ann Arbor, MI 48109, USA
Nucl Med Biol 30:293-302. 2003..These data better define the structure-activity relationships for cholinesterase radiotracers and provide lead compounds for (18)F- labeling... - In vivo butyrylcholinesterase activity is not increased in Alzheimer's disease synapsesDavid E Kuhl
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical Center, 1500 East Medical Center Drive, Ann Arbor, MI 48109, USA
Ann Neurol 59:13-20. 2006.... - Treatment effects on nigrostriatal projection integrity in partial 6-OHDA lesions: comparison of L-DOPA and pramipexoleElyse S Kemmerer
Neuroscience Program, The University of Michigan, Ann Arbor, MI, USA
Exp Neurol 183:81-6. 2003..There was no treatment effect on VMAT2 expression in the partially lesioned striatum and thus no differential effect of indirect versus direct dopamimetic treatment on nigrostriatal integrity... - Regulation of human affective responses by anterior cingulate and limbic mu-opioid neurotransmissionJon Kar Zubieta
Department of Psychiatry and Mental Health Research Institute, University of Michigan, 205 Zina Pitcher Place, Ann Arbor, MI 48109 0720, USA
Arch Gen Psychiatry 60:1145-53. 2003..The mu-opioid neurotransmitter system is distributed in, and thought to regulate the function of, brain regions centrally implicated in affective processing... - Evaluation of 18F-labeled acetylcholinesterase substrates as PET radiotracersXia Shao
Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical Center, Ann Arbor, MI 48109, USA
Bioorg Med Chem 13:869-75. 2005.... - (R)-N-[11C]methyl-3-pyrrolidyl benzilate, a high-affinity reversible radioligand for PET studies of the muscarinic acetylcholine receptorMarc B Skaddan
Department of Radiology, University of Michigan Medical School, Ann Arbor, Michigan 48109-0552, USA
Synapse 45:31-7. 2002..This pretreatment produced a modest, statistically significant decrease (9-11%) in the distribution volume ratios for muscarinic receptor rich regions of the rat brain as compared to controls... - Effects of buprenorphine maintenance dose on mu-opioid receptor availability, plasma concentrations, and antagonist blockade in heroin-dependent volunteersMark K Greenwald
Department of Psychiatry and Behavioral Neurosciences and Addiction Research Institute, Wayne State University, Detroit, MI 48207, USA
Neuropsychopharmacology 28:2000-9. 2003.... - mu-opioid receptor-mediated antinociceptive responses differ in men and womenJon-Kar Zubieta
Department of Psychiatry and Mental Health Research Institute, University of Michigan, Ann Arbor, Michigan 48109-0720, USA
J Neurosci 22:5100-7. 2002..These data demonstrate that at matched levels of pain intensity, men and women during their follicular phase differ in the magnitude and direction of response of the mu-opioid system in distinct brain nuclei... - Radiopharmaceutical spaceWilliam C Eckelman
Nucl Med Biol 33:829. 2006 - [11C]Glycylsarcosine: synthesis and in vivo evaluation as a PET tracer of PepT2 transporter function in kidney of PepT2 null and wild-type miceNabeel B Nabulsi
Division of Nuclear Medicine, Department of Radiology, School of Medicine, The University of Michigan, Ann Arbor, MI 48109, USA
Bioorg Med Chem 13:2993-3001. 2005..This study demonstrates using in vivo imaging technique that PepT2 is primarily responsible for renal tubular active reabsorption of Gly-Sar, and provides a new tool for studying tubular peptide reabsorption and clearance... - A simple method for stem cell labeling with fluorine 18Bing Ma
Department of Radiology, Division of Nuclear Medicine, University of Michigan Medical School, Ann Arbor, 48109, USA
Nucl Med Biol 32:701-5. 2005..18)F]HFB is thus simple to prepare and uses labeling agent for short-term distribution studies of injected stem cells... - Justifying the number of animals for each experimentWilliam C Eckelman
Nucl Med Biol 34:229-32. 2007 - Cognitive function and nigrostriatal markers in abstinent methamphetamine abusersChris Ellyn Johanson
Department of Psychiatry and Behavioral Neurosciences, Wayne State University, Detroit, MI 48207, USA
Psychopharmacology (Berl) 185:327-38. 2006..The present study was designed to further our understanding of changes in brain function in humans that might result from chronic high dose use of MA after at least 3 months of abstinence... - Discussion of targeting proteins in vivo: in vitro guidelinesWilliam C Eckelman
Nucl Med Biol 33:449-51. 2006
Research Grants
- NEW PET RADIOTRACERS--MONOAMINE REUPTAKE INHIBITORSMichael Kilbourn; Fiscal Year: 1993..New quantitative PET techniques for the study of the monoamine systems will permit direct evaluation of disease-related hypotheses in neurology, psychiatry, and drug abuse research...
- NEW PET RADIOTRACERS--MONOAMINE TRANSPORTERSMichael Kilbourn; Fiscal Year: 2000....
- New PET Radiotracers-Monoamine TransportersMichael Kilbourn; Fiscal Year: 2003....