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in creator/contributor: "VanBrocklin, Henry F."  
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Synthesis ofN-(2-chloro-5-methylthiophenyl)-N'-(3-methyl-thiophenyl)-N'-[3H3]methylguanidine, l brace [3H3]CNS-5161 r brace

Description: The preparation of the title compound, [{sup 3}H{sub 3}]CNS-5161, was accomplished in three steps starting with the production of [{sup 3}H{sub 3}]iodomethane (CT{sub 3}I). The intermediate N-[{sup 3}H{sub 3}]methyl-3-(thiomethylphenyl)cyanamide was prepared in 77% yield by the addition of CT{sub 3}I to 3-(thiomethylphenyl)cyanamide, previously treated with sodium hydride. Reaction of this tritiated intermediate with 2-chloro-5-thiomethylaniline hydrochloride formed the guanidine compound [{sup… more
Date: September 28, 2001
Creator: Gibbs, Andrew R.; Morimoto, Hiromi; VanBrocklin, Henry F.; Williams, Philip G. & Biegon, Anat
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Partner: UNT Libraries Government Documents Department
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Kinetic analysis of 18F-fluorodihydrorotenone as a deposited myocardial flow tracer: Comparison to thallium-201.

Description: The goal of this investigation was to assess the accuracy of 18F-fluorodihydrorotenone (18F-FDHR) as a new deposited myocardial flow tracer and compare the results to those for 201Tl. Methods. The kinetics of these flow tracers were evaluated in 22 isolated, erythrocyte- and albumin-perfused rabbit hearts over a flow range encountered in patients. The two flow tracers plus a vascular reference tracer (131I-albumin) were introduced as a bolus through a port just above the aortic cannula. Myocard… more
Date: March 1, 2004
Creator: Marshall, Robert C.; Powers-Risius, Patricia; Reutter, Bryan W.; O'Neil, James P.; La Belle, Michael; Huesman, Ronald H. et al.
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Partner: UNT Libraries Government Documents Department
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Synthesis of 6-acrylamido-4-(2-[18F]fluoroanilino)quinazoline: Aprospective irreversible EGFR binding probe

Description: Acrylamido-quinazolines substituted at the 6-position bindirreversibly to the intracellular ATP binding domain of the epidermalgrowth factor receptor (EGFR). A general route was developed forpreparing 6-substituted-4-anilinoquinazolines from [18F]fluoroanilinesfor evaluation as EGFR targeting agents with PET. By a cyclizationreaction, 2-[18F]fluoroaniline was reacted withN'-(2-cyano-4-nitrophenyl)-N,N-dimethylimidoformamide to produce6-nitro-4-(2-[18F]fluoroanilino)quinazoline in 27.5 percentde… more
Date: March 30, 2004
Creator: Vasdev, Neil; Dorff, Peter N.; Gibbs, Andrew R.; Nandanan,Erathodiyil; Reid, Leanne M.; O'Neil, James P. et al.
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Partner: UNT Libraries Government Documents Department
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A new precursor for the preparation of 6-[18F]-fluoro-L-m-tyrosine (FMT): Efficient synthesis and comparison of radiolabeling

Description: For the electrophilic preparation of 6-[18F]-Fluoro-L-m-tyrosine (FMT), a PET tracer for measuring changes in dopaminergic function in movement disorders, a novel precursor, N-(tert-butoxycarbonyl)-3-(tert-butoxycarbonyloxy)-6-trimethylstannnyl-L-phenylalanine ethyl ester, was synthesized in four steps and 26 percent yield starting from L-m-tyrosine. FMT produced by two methods at two institutions was comparable in decay corrected yield, 25-26 percent, and quality (chemical, enantiomeric, and r… more
Date: January 9, 2004
Creator: VanBrocklin, Henry F.; Blagoev, Milan; Hoepping, Alexander; O'Neil, James P.; Klose, Manuela; Schubiger, Pius A. et al.
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Partner: UNT Libraries Government Documents Department
open access

Dialkoxyquinazolines: Screening Epidermal Growth Factor ReceptorTyrosine Kinase Inhibitors for Potential Tumor Imaging Probes

Description: The epidermal growth factor receptor (EGFR), a long-standingdrug development target, is also a desirable target for imaging. Sixteendialkoxyquinazoline analogs, suitable for labeling with positron-emittingisotopes, have been synthesized and evaluated in a battery of in vitroassays to ascertain their chemical and biological properties. Thesecharacteristics provided the basis for the adoption of a selection schemato identify lead molecules for labeling and in vivo evaluation. A newEGFR tyrosine k… more
Date: September 1, 2005
Creator: VanBrocklin, Henry F.; Lim, John K.; Coffing, Stephanie L.; Hom,Darren L.; Negash, Kitaw; Ono, Michele Y. et al.
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Partner: UNT Libraries Government Documents Department
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