Research Topics
Species | Zhude TuSummaryAffiliation: Washington University School of Medicine Country: USA Publications
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Detail Information
Publications
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groupsZhude Tu
Department of Radiology, Washington University, St Louis, MO 63110, United States
Bioorg Med Chem 20:4422-9. 2012..2 nM, VAChT/σ(1)=1500, VAChT/σ(2)=2030). These four compounds can be radiosynthesized with C-11 or F-18 to validate their possibilities of serving as PET probes for quantifying the levels of VAChT in vivo...- Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brainZhude Tu
Department of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
Bioorg Med Chem 19:1666-73. 2011..MicroPET studies of [(11)C]MP-10 in monkeys displayed selective uptake in striatum. However, a radiolabeled metabolite capable of penetrating the blood-brain-barrier may limit the clinical utility of [(11)C]MP-10 as a PDE10A PET tracer... - Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporterZhude Tu
Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
J Med Chem 52:1358-69. 2009..88 at 30 min postinjection (p.i.). MicroPET imaging of macaques demonstrated a 2.1 ratio of (-)-[(18)F]9e in putamen versus cerebellum at 2 h p.i. (-)-[(18)F]9e has potential to be a PET tracer for clinical imaging of the VAChT... - Carbon-11 labeled papaverine as a PET tracer for imaging PDE10A: radiosynthesis, in vitro and in vivo evaluationZhude Tu
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
Nucl Med Biol 37:509-16. 2010..Analogs of papaverine having a higher potency for inhibiting PDE10A and improved pharmacokinetic properties will be necessary for imaging this enzyme with PET... 
Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomographyZhude Tu
Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
J Med Chem 50:3194-204. 2007....- Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: a positron emission tomography studyRobert H Mach
Division of Radiological Sciences, Washington University School of Medicine, Mallinckrodt Institute of Radiology, Missouri 63110, USA
Synapse 65:724-32. 2011..These data indicate that there is a high level of competition between [¹⁸F]5 and endogenous dopamine for D₃ receptors in vivo... - [3H]4-(dimethylamino)-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl) butyl)benzamide: a selective radioligand for dopamine D(3) receptors. II. Quantitative analysis of dopamine D(3) and D(2) receptor density ratio in the caudate-putamenJinbin Xu
Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri 63110, USA
Synapse 64:449-59. 2010..A mathematical model for calculating the absolute densities of dopamine D(2) and D(3) receptors based on the in vitro receptor binding data of [3H]WC-10 and [3H]raclopride was developed... - Synthesis and in vivo evaluation of 2 high-affinity 76Br-labeled sigma2-receptor ligandsDouglas J Rowland
Department of Radiology, Washington University in St Louis, Saint Louis, Missouri, USA
J Nucl Med 47:1041-8. 2006..These are 5-bromo-N-(4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide (compound (1)) and 5-bromo-N-(2-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)ethyl)-2-methoxybenzamide (compound (2))... - Effect of cyclosporin A on the uptake of D3-selective PET radiotracers in rat brainZhude Tu
Department of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
Nucl Med Biol 38:725-39. 2011..Four benzamide analogs having a high affinity and selectivity for D(3) versus D(2) receptors were radiolabeled with (11)C or (18)F for in vivo evaluation... - [(3)H]4-(Dimethylamino)-N-[4-(4-(2-methoxyphenyl)piperazin- 1-yl)butyl]benzamide, a selective radioligand for dopamine D(3) receptors. I. In vitro characterizationJinbin Xu
Department of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, USA
Synapse 63:717-28. 2009..In vitro autoradiography studies of rat and monkey brains show that [(3)H]WC-10 labeled D(3) sites in the striatal region... - Radiosynthesis and biological evaluation of a promising sigma(2)-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancerZhude Tu
Division of Radiological Sciences, Washington University School of Medicine, Campus Box 8225, 510 South Kingshighway Blvd, St Louis, MO 63110, USA
Appl Radiat Isot 68:2268-73. 2010.... - Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligandsZhude Tu
Department of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, United States
J Med Chem 54:1555-64. 2011..17 nM for D(3), 163-fold selectivity for D(3) vs D(2) receptors), represents a candidate fluorine-18 radiotracer for in vivo PET imaging studies on the regulation of D(3) receptor expression... - Synthesis, radiolabeling and initial in vivo evaluation of [(11)C]KSM-01 for imaging PPAR-α receptorsKiran Kumar Solingapuram Sai
Division of Radiological Sciences, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
Bioorg Med Chem Lett 22:6233-6. 2012..5-fold greater radiotracer uptake in the heart of transgenic mice compared to the wild-type littermates. These results demonstrate the potential utility of PPAR-α agonists as PET radiopharmaceuticals... - Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptorsWei Wang
Department of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, United States
J Med Chem 54:5362-72. 2011..All four of these most promising compounds (14a, 14b, 14c, and 14e) can be radiosynthesized with fluorine-18 or carbon-11, which will allow further evaluation of their properties as PET probes for imaging σ(1) receptor in vivo... - Synthesis and characterization of selective dopamine D2 receptor antagonistsSuwanna Vangveravong
Division of Radiological Sciences, Washington University School of Medicine, Mallinckrodt Institute of Radiology, St. Louis, MO 63110, USA
Bioorg Med Chem 14:815-25. 2006.... 
Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonistJinbin Xu
Department of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
Neuroimage 71:168-74. 2013..d-Amphetamine challenge studies indicate that there is a significant displacement of [(11)C]SV-III-130 by d-Amphetamine-induced increases in synaptic dopamine levels...- Synthesis and evaluation of 15-(4-(2-[¹⁸F]Fluoroethoxy)phenyl)pentadecanoic acid: a potential PET tracer for studying myocardial fatty acid metabolismZhude Tu
Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
Bioconjug Chem 21:2313-9. 2010..0030 ± 0.0005 vs 0.0006 ± 0.00013, P < 0.01). These initial studies suggest that [¹⁸F]7 could be a potentially useful clinical PET tracer to assess abnormal myocardial fatty acid metabolism... - [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probeJinbin Xu
Department of Radiology, Washington University School of Medicine, 510 S. Kingshighway Blvd, St. Louis, MO 63110, USA
Eur J Pharmacol 525:8-17. 2005..The pharmacologic profile of [3H]RHM-1 was in agreement with that of [3H]DTG. The results of this study indicate that [3H]RHM-1 is a useful ligand for studying sigma2 receptors in vitro... - Identification of the PGRMC1 protein complex as the putative sigma-2 receptor binding siteJinbin Xu
Division of Radiological Sciences, Department of Radiology, Mail Box 8225, Washington University School of Medicine, 510 S Kingshighway Boulevard, St Louis, Missouri 63110, USA
Nat Commun 2:380. 2011..The identification of the putative sigma-2 receptor-binding site as PGRMC1 should stimulate the development of unique imaging agents and cancer therapeutics that target the sigma-2 receptor/PGRMC1 complex... - Binding of the radioligand SIL23 to α-synuclein fibrils in Parkinson disease brain tissue establishes feasibility and screening approaches for developing a Parkinson disease imaging agentDevika P Bagchi
Department of Neurology, Washington University School of Medicine, St Louis, MO, USA
PLoS ONE 8:e55031. 2013.... - Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10AZhanbin Zhang
Mallinckrodt Institute of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
Eur J Med Chem 46:3986-95. 2011..To identify high potent PDE10A inhibitor, further optimization of the structures of these analogues is necessary... - Characterization of a novel iodinated sigma-2 receptor ligand as a cell proliferation markerCatherine Hou
Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
Nucl Med Biol 33:203-9. 2006..Further modification of the ligand and the imaging parameters will be needed to improve the signal for in vivo detection... - Synthesis and in vivo evaluation of [11C]PJ34, a potential radiotracer for imaging the role of PARP-1 in necrosisZhude Tu
Division of Radiological Sciences, Washington University School of Medicine, St. Louis, MO 63110, USA
Nucl Med Biol 32:437-43. 2005..These data indicate that [(11)C]PJ34 may be a useful radiotracer for imaging tissues undergoing cellular death via necrosis... - Automated radiosynthesis of [11C]morphine for clinical investigationJinda Fan
Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Blvd St Louis, MO 63110, USA
Appl Radiat Isot 69:431-5. 2011..Radiosynthesis took 45 min with a radiochemical yield ranging from 45% to 50% and specific activity ranging from 20 to 26 Ci/μmol (decay corrected to end-of-bombardment); radiochemical and chemical purities were >95% (n=28)... - Chemical and enzyme-assisted syntheses of norbuprenorphine-3-β-D-glucuronideJinda Fan
Department of Radiology, Washington University in St Louis, 660 S Euclid Avenue, St Louis, Missouri 63110, United States
Bioconjug Chem 22:752-8. 2011..The fractional yield of the enzyme-assisted synthesis was greater than that of the chemical synthesis (67% vs 5.3%), but due to larger reaction volumes, the chemical synthesis afforded greater amounts of total 1... - N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studiesWenhua Chu
Division of Radiological Sciences, Washington University School of Medicine, 510 South Kingshighway Boulevard, St. Louis, Missouri 63110, USA
J Med Chem 48:7637-47. 2005.... - Carbon-11 labeled sigma2 receptor ligands for imaging breast cancerZhude Tu
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA
Nucl Med Biol 32:423-30. 2005..Consequently, [(11)C]2 is a potential radiotracer for imaging the proliferative status of breast tumors in vivo with PET... - Synthesis and in vitro evaluation of α-synuclein ligandsLihai Yu
Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard, St Louis, MO 63110, USA
Bioorg Med Chem 20:4625-34. 2012..Further optimization of the structure of these analogues may yield compounds with high affinity and selectivity for aggregated α-synuclein... - The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabineJohn R Hornick
Department of Surgery, Washington University School of Medicine, S, Euclid Avenue, St Louis, MO, USA
Mol Cancer 9:298. 2010..In this study, we investigated the role of the novel sigma-2 receptor ligand SW43 to induce apoptosis and augment standard chemotherapy... - Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligandsWenhua Chu
Department of Radiology, Division of Radiological Sciences, Washington University School of Medicine, Campus Box 8225, 510 S. Kingshighway Blvd, St. Louis, MO 63110, USA
Bioorg Med Chem 13:77-87. 2005....